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A Contract Research and Development Company
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Publications
2012
"3-Substituted Pyrazole Analogs of the Cannabinoid Type 1 (CB1) Receptor Antagonist Rimonabant: Cannabinoid Agonist-Like Effects in Mice via Non-CB1, Non-CB2 Mechanism", Wiley, J. L.; Selley, D. E.; Wang, P.; Kottani, R.; Gadthula, S.; Mahadevan, A.; J. Pharmacol. Exper.Ther., 2012, 340(2), 433.
2011
"Δ8-Tetrahydrocannabivarin protects against hepatic ischemia/reperfusion injury by attenuating oxidative stress and inflammatory response involving CB2 receptors ", Batkai, S.; Mukhopadhyay, P.; Horvath, B.; Rajesh, M.; Gao, R. Y.; Mahadevan, A.; Amere, M.; Battista, N.; Lichtman, A. H.; Gauson, L. A.; Maccarrone, M.; Pertwee, R. G.; Pacher, P.; Br. J. Pharmacol ., 2011, 6.
"Inhibition of monoacylglycerol lipase (MAGL) attenuates NSAID-induced gastrichemorrhages in mice ", Kinsey, S. G.; O’Neal, S. T.; Nomura, D. K.; Long, J. Z.; Mahadevan, A.; Cravatt, B. F.; Grider, J. R.; Lichtman, A. H.; J. Pharmacol. Exper.Ther ., 2011, 338(3), 795.
"The synthesis and biological evaluation of 2-(3-methyl or 3-phenylisoxazol-5-yl)-3-aryl-8-thiabicyclo[3.2.1]octanes", Purushotham, M.; Sheri, A.; Pham-Huu, D-P.; Madras, B. K.; Janowsky, A.; Meltzer, P.C.; Bioorg. & Med. Chem. Lett., 2011, 21, 48.
"The CB2 cannabinoid receptor-selective agonist O-3223 reduces pain and inflammation without apparent cannabinoid behavioral effects", Kinsey, S. G.; Mahadevan, A.; Zhao, B.; Sun, H.; Naidu, P. S.; Razdan, R. K.; Selley, D. E.; Imad Damaj, M.; Lichtman, A. H.; Neuropharmacology, 2011, 60, 244.
"Structural and pharmacological analysis of O-2050, a putative neutral cannabinoid CB1 receptor antagonist", Wiley, J. L.; Breivogel, C. S.; Mahadevan, A.; Pertwee, R. G.; Cascio, M. G.; Bolognini, D.; Huffman, J. W.; Walentiny, M. D.; Vann, R. E.; Razdan, R. K.; Martin, B. R.; Eur. J. Pharmacol., 2011, 651, 96.
2009
"Evaluation of prevalent phytocannabinoids in the acetic acid model of visceral nociception", Booker, L.; Naidu, P. S.; Razdan, R. K.; Mahadevan, A.; Lichtman, A. H. Drug Alcohol Depend. 2009, 105, 1.
"Synthesis and pharmacological activity of a potent inhibitor of the biosynthesis of the endocannabinoid 2-arachidonylglycerol", Bisogno, T.; Burston, J. J.; Rai, R.; Allara, M.; Saha, B.; Mahadevan, A.; Razdan, R. K.; Wiley, J. L.; DiMarzo, V. Chem. Med. Chem., 2009 4, 946.
2008
"Multiple pathways involved in the biosynthesis of anandamide", J. Liu, L. Wang, J. Harvey-White, B. X. Huang, H. Y. Kim, S. Luquet, R. D. Palmiter, G. Krystal, R. Rai, A. Mahadevan, R. K. Razdan, G. Kunos. Neuropharmacology. 2008, 54, 1, 1.
"Synthesis of 2-(5Z,8Z,11Z,14Z)-icosa-5,8,11,14-tetraenamidoethyl-d4 dihydrogen phosphate, tetra-deuterated pAEA", K. Cheng, B. Saha, A. Mahadevan, R. K. Razdan, G. Kunos, A. E. Jacobson, K. C. Rice. J. Label Compd. Radiopharm. 2008, 51, 389.
"The synthesis of bivalent 2β-carbomethoxy-3β-(3,4-dichlorophenyl)-8-heterobicyclo[3.2.1]octanes as probes for proximal binding sites on the dopamine and serotonin transporters", P. C. Meltzer, O. Kryatova, D-P. Pham-Huu, P. Donovan, A. Janowsky. Bioorg. & Med. Chem.,16, 1832-1841 2008.
2007
"The role of fluorine substitution in the structure-activity relationships (SAR) of classical cannabinoids", P. J. Crocker, A. Mahadevan, J. L. Wiley, B. R. Martin, R. K. Razdan. Bioorg. Med. Chem. Lett. 2007, 17, 1504.
"Synthesis of 8-thiabicyclo[3.2.1]octanes and their binding affinity for the dopamine and serotonin transporters”, D-P. Pham-Huu, J. R. Deschamps, S. Liu, B. K. Madras and P. C. Meltzer, Bioorg. & Med. Chem. 15, 1067-1082, 2007.
"Novel, potent THC/anandamide (hybrid) analogs", C. Bourne, S. Roy, J. L. Wiley, B. R. Martin, B. F. Thomas, A. Mahadevan, R. K. Razdan. Bioorg. Med. Chem. 2007, 15, 7850.
2006
"Inhibition of Cytosolic
Phospholipase A2a: Hit to Lead Optimization", J. C.
McKew, M. A. Foley, P. Thakker, M. L. Behnke, F. E. Lovering, F-W. Sum,
S. Tam, K. Wu, M. W. H. Shen, W. Zhang, M. Gonzalez, S. Liu, A. Mahadevan,
H. Sard, J. Med. Chem. 2006, 49, 135
"Novel compounds that
interact with both Leukotriene B4 receptors and vanilloid
TRPV1 receptors", D. McHugh, R. S. McMaster, R. G. Pertwee, S.
Roy, A. Mahadevan, R. K. Razdan, R. A. Ross, J. Pharmacol. Exper. Ther.
2006, 316, 955.
"Synthesis of 3-(4-Heteroaryl-phenyl)-8-oxabicyclo[3.2.1]octane-2-carboxylic
Acid Methyl Esters" L. Torun,
S. Liu, B. K. Madras and P. Meltzer, Tet. Lett. 47, 599-603,2006.
"1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one(Pyrovalerone)
analogs. A promising class of monoamine uptake inhibitors"P. C. Meltzer, D. Butler, J. R. Deschamps and B. K. Madras,
J. Med. Chem. 49, 1420-1432, 2006.
"New Potent and Selective
Inhibitors of Anandamide Re-Uptake with Anti-Spastic Activity in a Mouse
Model of Multiple Sclerosis", Ligresti, A.; Cascio, M. G.; Pryce,
G.; Kulasegram, S.; Beletskaya, I.; De Petrocellis, L.; Saha, B.; Mahadevan,
A.; Visintin, C.; Wiley, J. L.; Baker, D.; Martin, B. R.; Razdan, R.
K.; Di Marzo, V. Br. J. Pharmacol. 2006, 147,
83-91.
2005
"SAR of Psilocybin
Analogs: Discovery of a Selective 5-HT2C Agonist" H.
Sard, G. Kumaran, C. Morency, B. Roth, B. Toth, P. He, and L.
Shuster Bioorg. Med. Chem. Lett. 15, 4555, 2005.
"The search for cocaine pharmacotherapies continues: Analogs
of pyrrolidinyltolylpentanone (pyrovalerone) are potent inhibitors of
monoamine transport", P. C. Meltzer,
D. Butler, J. R. Deschamps and B. K. Madras, College on Problems of
Drug Dependence, Florida, 2005.
"CB1 Cannabinoid Receptor-Mediated
modulation of Food Intake in Mice", J. L. Wiley, J. J. Burston,
D. C. Leggett, R. K. Razdan, A. Mahadevan, B. R. Martin, Br. J. Pharmacol.
2005, 145, 293.
"Influence of the
degree of unsaturation of the acyl side chain upon the interaction of
analogues of 1-arachidonylglycerol with monoglycerol lipase and fatty
acid amide hydrolase", S. Vandevoorde, B. Saha, A. Mahadevan, R.
K. Razdan, R. G. Pertwee, B. R. Martin, C. J. Fowler, Biochem. Biophys.
Res. Commun. 2005, 337, 104.
"Further Advances
in the Synthesis of Endocannabinoid-related Ligands", A. Mahadevan,
R. K. Razdan, AAPS 2005, 07(02), E496.
"Inhibition of leukocyte
function and interleukin-2 gene expression by 2-methylarachidonyl-(2Õ-fluoroethyl)amide,
a stable congener of the endogenous cannabinoid receptor ligand anandamide",
Kaplan, B. L. F.; Ouyang, Y.; Herring, A.; Yea, S. S.; Razdan, R.; Kaminski,
N. E. Toxicol. Appl. Pharmacol. 2005, 205, 107-115.
"Task specificity
of cross-tolerence between D9-tetrahydrocannabinol and anandamide analogs in mice",
Wiley, J. L.; Smith, F. L.; Razdan, R. K.; Dewey, W. L. Eur. J. Pharmacol.
2005, 510, 59-68.
"Synthesis of novel 5-substituted
pyrazole derivatives as cannabinoid antagonists", Alekseeva, O. O.;
Mahadevan, A.; Wiley, J. L.; Martin, B. R.; Razdan. R. K. Tet. Lett.
2005, 46, 2159-2161.
"CB1 cannabinoid receptor-mediated
modulation of food intake in mice", Wiley, J. L.; Burston, J. J.;
Leggett, D. C.; Alekseeva, O. O.; Razdan, R. K.; Mahadevan, A.; Martin,
B. R. Br. J. Pharmacol. 2005, 145, 293-300.
2004
"DAT Imaging: From Speculative to Spectacular", P. C. Meltzer, and B. K.
Madras, NIDA Monog. 184, 76-79, 2004.
"Synthesis
of 8-thiabicyclo[3.2.1]oct-2-enes and their binding affinity for the
dopamine and serotonin transporters", P. C. Meltzer, D-P. Pham-Huu, and B. K. Madras Bioorg. & Med. Chem. Lett. 14, 6007-6010, 2004.
"A new class of potent inhibitors of monoamine transport: 8-thiabicyclo[3.2.1]oct-2-enes",
P. C. Meltzer, P. Pham-Huu, and B. K. Madras, College on Problems of
Drug Dependence, Puerto Rico, 2004.
"A Novel Methodology
for the Synthesis of 1-desoxy-Δ8-tetrahydrocannabinol
(THC) analogues", H. Sun, A. Mahadevan, R. K. Razdan, Tet. Lett.
2004, 45, 615
"A Comparison of the
Discriminative Stimulus Effects Δ9-Tetrahydrocannabinol
and O-1812, a Potent and Metabolically Stable Anandamide Analog, in
Rats", J. L. Wiley, K. L. LaVecchia, N. E. Karp, S. Kulasegaram,
A. Mahadevan, R. K. Razdan, B. R. Martin, Experimental and Clinical
Psychopharmacology 2004, 12, 173
"Inhibition of Monoacylglycerol
Lipase and Fatty Acid Amide Hydrolase by Analogues of 2-Arachidonylglycerol",
N. Ghafouri, G. Tiger, R. K. Razdan, A. Mahadevan, R. G. Pertwee, B.
R. Martin, C. J. Fowler, Br. J. Pharmacol. 2004, 143,774.
"6"-Azidohex-2"-yne-cannabidiol:
a potential neutral, competitive cannabinoid CB1 receptor antagonist",
Thomas, A.; Ross, R. A.; Saha, B.; Mahadevan, A.; Razdan, R. K.; Pertwee,
R. G. Eur. J. Pharmacol. 2004, 487,
213-221
"A synthetic route
to anandamide analogues carrying a substituent at the terminal carbon
and an acetylene group in the end pentyl chain", Altundas, R.;
Mahadevan, A.; Razdan, R. K. Tet. Lett. 2004, 45, 5449-5451
2003
"Synthesis and evaluation of dopamine
and serotonin transporter inhibition by oxacyclic and carbacyclic analogues
of methylphenidate". P. C. Meltzer, P. Wang, P. Blundell, and B.
K. Madras. J. Med. Chem. 46, 1538, 2003.
"A
Second Generation 99mTechnetium SPECT Agent That Provides In VivoImages of the Dopamine Transporter in Primate
Brain" P. C. Meltzer, P. Blundell, T. Zona, L. Yang, H. Huang,
A. A. Bonab, E. Livni, A. Fischman and B. K. Madras. J. Med. Chem. 46,
3483, 2003.
"Synthesis
and Biological Activity of 2-Carbomethoxy-3-catechol-8-azabicyclo[3.2.1]octanes"
P. C. Meltzer, M. McPhee and B. K. Madras, Bioorg.
& Med. Chem. Lett. 13, 4133-4137, 2003.
"Non-amine-based
dopamine transporter (reuptake) inhibitors retain properties of amine-based
progenitors" B. K. Madras, M. A. Fahey, G. M. Miller, R. DeLa Garza,
M. Goulet, R. D. Spealman, P. C. Meltzer, S. R. George, B. F. O'Dowd,
A. A. Bonab, E. Livni, A. J. Fischman, Eur. Journal Pharm. 479, 41-51,
2003.
"A General Method
for C3 Reductive Alkylation of Indoles"A.Mahadevan, H. Sard, M.
Gonzalez, and J. McKew, Tetrahedron Letters 44,
4589, 2003.
"Selective
ligands and cellular effectors of a G protein-coupled endothelial cannabinoid
receptor", Offertaler, L.; Mo, F-M.; Batkai, S.; Liu, J.; Begg,
M.; Razdan, R. K.; Martin, B. R.; Bukoski, R. D.; Kunos, G. Mol. Pharm.
2003, 63, 699-705.
2002
"Dopamine transporter occupancy by candidate cocaine medications".
B. K. Madras, P. C. Meltzer, A. A. Bonab, E. Livni, and A. J. Fischman.
J. Nucl. Med. 43, 232, 2002.
"Evaluation of dopamine transporter (DAT) density in patients
with parkinson's disease (PD) by PET with 127I, 11C altropane".
A. J. Fischman, A. A. Bonab, E. Livni, P. C. Meltzer, S. A. Barrow,
and B. K. Madras,. J. Nucl. Med. 43, 18, 2002.
"The Tropane Horse: A novel cocaine antagonist strategy?"
B. K. Madras, J. T. Bendor, A. R. Meyerhoff, G. M. Miller, and P. C.
Meltzer. Drug and Alcohol Dependence", 60, S109:406, 2002.
"Non-amines: A generalization to methylphenidate and indatraline".
P. C. Meltzer, P. Blundell, and B. K. Madras, Drug and Alcohol Dependence",
60, S118:441, 2002.
"The therapeutic potential of a dopamine transporter (DAT) inhibitor
for Parkinson's disease: Comparison with AD2 dopamine agonist in MPTP-treated
monkeys". B. K. Madras, P. C. Meltzer, and M. Goulet. Soc. Neurosc.,
in press.
" Design and synthesis of an irreversible dopamine-sparing cocaine
antagonist" P. C. Meltzer, S. Liu, H. S. Blanchette, P. Blundell,
and B. K. Madras. Bioorg. & Med. Chem. 10, 3583, 2002.
"Assessment
of structural commonality between tetrahydrocannabinol and anandamide",
Martin, B. R.;.Jefferson, R. G.; Winckler, R.; Wiley, J. L.; Thomas,
B. R.; Crocker, P. J.; Williams, W.; Razdan, R. K. Eur. J. Pharmacol.
2002, 435, 35-42.
"A
Structure/Activity Relationship Study on Arvanil, an Endocannabinoid
and Vanilloid Hybrid", DiMarzo, V.; Griffin, G.; DePetrocellis,
L.; Brandi, I.; Bisogno, T.; Williams, W.; Grier, M. C.; Kulasegram,
S.; Mahadevan, A.; Razdan, R. K.; Martin, B. R. J. Pharmacol. Expt.
Ther. 2002, 300, 984-991.
"Resorcinol
Derivatives: A Novel Template for the Development of Cannabinoid CB1/CB2 and CB2-Selective Agonists", Wiley, J. L.; Beletskaya,
I. D.; Ng, E. D.; Zongmin, D.; Crocker, P.J.; Mahadevan, A.; Razdan,
R. K.; Martin, B. R. J. Pharmacol. Expt. Ther. 2002, 301 679-689.
"Recent
advances in the synthesis of endocannabinoid related ligands",
Razdan, R. K. and Mahadevan, A. Chem. Phys. Lipids, 2002, 121/1-2, 21-33.
"SR-141716A-induced
stimulation of locomotor activity; A Structure-activity relationship
study", Bass, C. E.; Griffin, G.; Grier, M.; Mahadevan, A.; Razdan,
R. K.; Martin, B. R. Pharmacol. Biochem. Behav. 2002, 74, 31-40.
2001
"Non-amines, drugs without an amine nitrogen, potently block
serotonin transport (reuptake): novel anti-depressant candidates?",
M. Goulet, G. M. Miller, P. C. Meltzer, B. K. Madras. Synapse, 42, 129-140,
2001.
"[(11)C, (127)I] Altropane: a highly selective ligand for PET
imaging of dopamine transporter sites", Fischman, A. J, Bonab,
A. A, Babich, J. W, Livni, E, Alpert, N. M. Meltzer, P. C, Madras, B.
K. Synapse, 39, 332-342. 2001.
"A tropane horse I. Design and synthesis of a dopamine sparing
antagonist", P. C. Meltzer, P. Blundell, S. Liu, H. Blanchette
and B. K. Madras, Drug and Alcohol Dependence, 63, 414, 2001.
"A tropane horse II. O-1893 interferes with cocaine binding
but permits dopamine transport: a cocaine antagonist strategy?"
B. K. Madras, P. Blundell, S. Liu and P. C. Meltzer, Drug and Alcohol
Dependence, 63, 378, 2001.
"Synthesis of 6- and 7-hydroxy-8-azabicyclo[3.2.1]octanes and
their binding affinity for the dopamine and serotonin transporters",
P. C. Meltzer, B. Wang, Z. Chen, P. Blundell, M. Jayaraman, M. D. Gonzalez,
C. George, and B. K. Madras, J. Med. Chem., 44, 2619-2635, 2001.
"Human DAT binding measurement with 11C-altropane", A.
A. Bonab, N. M. Alpert, E. Livni, P. C. Meltzer, B. K. Madras, and A.
J. Fischman. J. Nucl. Med. 42, 184, 2001.
"Human brain SPECT imaging wit a highly selective DAT ligand
99mTc-O-1505T". A. A. Bonab, P. C. Meltzer, N. M. Alpert, M. Burker,
S. D. Dragotakes, B. Barrow, B. K. Madras, and A. J. Fischman. J. Nucl.
Med. 42, 210, 2001.
"Occupancy of the dopamine transporter by a transporter inhibitor,
as measured by PET imaging, is predictive of therapeutic efficacy for
Parkinsonism". B. K. Madras, P. C. Meltzer, J. W. Babich, A. A.
Bonab, and A. J. Fischman. J. Nucl. Med. 42, 210, 2001.
"Highly
Selective CB1 Cannabinoid Receptor ligands and Novel CB1/VR1 Vanilloid
Receptor "Hybrid Ligands", DiMarzo, V.; Bisogno, T.; DePetrocellis,
L.; Brandi, I.; Jefferson, R. G.; Winckler, R. L.; Davis, J. B.; Dasse,
O.; Mahadevan, A.; Razdan, R. K.; Martin, B. R. Biochem. Biophys. Res.
Commun. 2001, 281, 444-451.
"Novel
Pyrazole Cannabinoids: Insights into CB1 Receptor Recognition and Activation",
Wiley, J. L.; Jefferson, R. G.; Grier, M. C.; Mahadevan, A.;. Razdan,
R. K.; Martin, B. R. J. Pharmacol. Exp. Ther. 2001, 296, 1013-1022.
2000
"Preparation of 4,5-Disubstituted Pyrimidines: Ring Substitution
of 5-Mesyloxymethylpyrimidines" H. Sard, M. Gonzalez, A. Mahadevan,
and J. McKew, J. Org. Chem. 65, 9261, 2000.
"[11C]Tropoxene: a dopamine transport inhibitor that bears no
amine nitrogen, accumulates in the dopamine-rich striatum of monkey:
a PET study", Madras B. K, Meltzer P. C, Bonab A. A, Livni, Babich
J. W, Fischman A. J. J. Nucl. Med. 41: 208, 2000.
"3-Aryl-2-carbomethoxybicyclo[3.2.1]oct-2-enes Inhibit WIN 35,428
Binding and Selectively at the Dopamine Transporter", P. C. Meltzer,
P. Blundell, H. Huang, S. Liu, Y. F. Yong, and B. K. Madras, Bioorganic
& Medicinal Chemistry, 8, 581-590, 2000.
"2-Carbomethoxy-3-aryl-8-bicyclo[3.2.1]octanes: potent non-nitrogen
inhibitors of monoamine transporters", P. C. Meltzer, P. Blundell,
Y. F. Yong, Z. Chen, C. George, M. D. Gonzalez, and B. K. Madras J.
Med. Chem., 43, 2982-2991, 2000.
"QSAR Analysis of Δ8-THC Analogues: Relationship of Side-Chain
Conformation to Cannabinoid Receptor Affinity and Pharmacological Potency",
Keimowitz, A. R.; Martin, B. R.; Razdan, R. K.; Crocker, P. J.; Mascarella,
S. W.; Thomas, B. F. J. Med. Chem. 2000, 43, 59.
"Cardiovascular Effects of 2-Arachidonyl Glycerol in Anesthetized
Mice", Zolton, J.; Wagner, J. A.; Goparaju, S. K.; Wang, L.; Razdan,
R. K.; Sugiura, T.; Zimmer, A. M.; Bonner, T. I.; Zimmer, A.; Kunos,
G. Hypertension, 2000, 35, 679.
"Molecular and regional targets of cocaine in primate brain:
liberation from prosaic views. Addiction Biology", Madras B. K,
Miller G. M., Meltzer P. C., Brownell A-L, Fischman A. J, Addiction
Biology, 5, 351-359, 2000.
"Association of psychostimulants on the dopamine transporter:
Biochemical and molecular evidence for multiple binding domains",
B. K. Madras, M. A. Fahey, P. C. Meltzer, G. M. Miller, Drug and Alcohol
Dependence, 60, 383, 2000
"Quantification of SPECT imaging with a highly selective DAT
ligand 99mTc-O-1505". A. A. Bonab, P. C. Meltzer, S. Hillier, M.
Burker, S. A. Barrow, B. K. Madras, and A. J. Fischman. J. Nucl. Med.
41, 185, 2000.
"Radiolabeling of the highly selective DAT ligand, Tc-O-1505,
with 99mTc. Choice of transchelation agent". S. Hillier, M. Burker,
P. C. Meltzer, B. K. Madras, and A. J. Fischman. J. Nucl. Med. 41, 185,
2000.
"Levels,
Metabolism, and Pharmacological Activity of Anandamide in CB1 Cannabinoid
Receptor Knockout Mice: Evidence for Non-CB1, and Non-CB2 Receptor-Mediated
Actions of Ananadamide in Mouse Brain", DiMarzo, V.; Breivogel,
C. S.; Tao, Q.; Bridgen, D. T.; Razdan, R. K.; Zimmer, A. M.; Zimmer,
A.; Martin, B. R. J. Neurochem. 2000, 75, 2434-2444.
"The
Synthesis of N-Vanillyl-arachidonoyl-amide (Arvanil) and its Analogs:
An Improved Procedure for the Synthesis of the Key Synthon Methyl 14-Hydroxy-(all-cis)-5,8,11,-Tetradecatrienonate",Dasse, O.; Mahadevan,
A.; Han, L.; Martin, B. R.; DiMarzo, V.; Razdan, R. K. Tetrahedron,
2000, 56, 9195-9202.
1999
"Total Synthesis of 2-Arachidonylglycerol (2-Ara-Gl)",
Han, L. and Razdan, R. K. Tet. Lett. 1999, 40, 1631.
"Unique Analogues of Anandamide: Arachidonyl Ethers and Carbamates
and Norarachidonyl Carbamates and Ureas", Ng, E. W.; Aung, M. M.;
Abood, M. E.; Martin, B. R.; Razdan, R. K. J. Med. Chem. 1999, 42, 1975.
"An Investigation into the structural determinants of cannabinoid
receptor ligand efficacy", Griffin, G.; Wray, E. J.; Rorrer, W.
K.; Crocker, P. J.; Saha, B.; Razdan, R. K.; Martin, B. R.; Abood, M.
E. Br.J. Pharmacol. 1999, 126, 1575.
"Manipulation of the Tetrahydrocannabinol Side Chain Delineates
Agonists, Partial Agonists, and Antagonists", Martin, B. R.; Jefferson,
R.; Winckler, R.; Wiley, J. L.; Huffman, J. W.; Crocker, P. J.; Saha,
B.; Razdan, R. K. J. Pharm. Exp. Ther. 1999, 290, 1065.
"Discovery and Characterization of Endogenous Cannabinoids",
Martin, B. R.; Mechoulam, R.; Razdan, R. K. Life Sci. 1999, 65, 573.
"Development of Agonists, Partial Agonists and Antagonists in
the Δ8-Tetrahydrocannabinol Series", Crocker, P. J. ;Saha, B.;
Ryan, W. J.; Wiley, J. L.; Martin, B. R.; Ross, R. A.; Pertwee, R. G.;
Razdan, R. K. Tetrahedron, 1999, 55, 13907.
"Structural determinants of the partial agonist-inverse agonist
properties of 6'-azidohex-2'-yne-Δ8-Tetrahydrocannabinol at cannabinoid
receptors", Ross, R. A.; Gibson, T. M.; Stevenson, L. A.; Saha,
B.; Crocker, P.; Razdan, R. K.; Pertwee, R. G. Br. J. Pharmacol. 1999,
128, 735.
"Cannabinoid induced mesentric vasodilation through an endothelial
site distinct from CB1 or CB2 receptors", Zolton, J.; Wagner, J.
A.; Varga, K.; lake, K. D.; Compton, D. R.; Martin, B. R.; Zimmer, A.
M.; Bonner, T. I.; Brickley, N. E.; Mezey, E.; Razdan, R. K.; Zimmer,
A.; Kunos, G. Proc. Natl. Acad. Sci. USA, 1999, 96, 14136.
"Bicyclo[3.2.1]octanes: Synthesis and Inhibition of Binding
at the Dopamine and Serotonin Transporters", P. C. Meltzer, P.
Blundell, Z. Chen, Y. Yong, and B. K. Madras, Bioorg. & Med. Chem.
Lett., 9, 857-862, 1999.
"Non-amine dopamine transporter probe [3H]Tropoxene distributes
to dopamine-rich regions in monkey brain", R. de la Garza. II,
P. C. Meltzer, and B. K. Madras, Synapse, 34, 20-27, 1999.
"Point mutations of the human dopamine transporter (hDAT) reveal
differential binding of an amine and a non-amine ligand", G. M.
Miller, L. M. Gracz, M. Goulet, H. Yang, P. C. Meltzer, B. J. Hoffman,
and B. K. Madras, Soc Neurosci Abstr. 25, 283, 1999.
"Non-amines: a new generation of transporter drugs are potent
serotonin reuptake blockers", Goulet M, Miller G. M, Meltzer P.
C., Madras B. K. Soc Neurosci Abstr. 25, 283, 1999
1998
"Total Synthesis of Methyl 14-Hydroxy-(all-cis)-5,8,11,-Tetradecatrienoate:
A Useful Intermediate For the Synthesis of Arachidonic Acid Analogues",
Han, L. and Razdan, R. K. Tetrahedron Lett. 1998, 39, 771.
"Potent Cyano and Carboxamido Side-Chain Analogues of 1',1'-Dimethyl-Δ8-Tetrahydrocannabinol,"
Singer, M.; Ryan, W. J.; Saha, B.; Martin, B. R.; Razdan, R. K. J. Med.Chem.
1998, 41, 4400.
"Comparison of Cannabinoid binding sites in guinea-pig forebrain
and small intestine" Ross, R. A.; Brockie, H. C.; Fernando, S.
R.; Saha, B.; Razdan, R. K.; Pertwee, R. G. Br.J. Pharmacol. 1998, 125,
1345.
"Anandamide, an Endogenous Cannabinoid, Has a very low Physical
Dependence Potential", Aceto, M. D.; Scates, S. M.; Razdan, R.
K.; Martin, B. R. J. Pharm. Exp. Ther. 1998, 287, 598.
"Evaluation of Cannabimimetic effects of structural analogs
of anandamide in rats", Wiley, J. L.; Ryan, W. J.; Razdan, R. K.;
Martin, B. R. Eur. J. Pharmacol. 1998, 355, 113.
"Altropane, a SPECT or PET Imaging Probe for Dopamine Neurons:
I. Dopamine Transporter Binding in Primate Brain", B. K. Madras,
P. C. Meltzer, A Y. Liang, D. R. Elmaleh, J. W. Babich, and A. J. Fischman,
Synapse, 29, 93-104, 1998.
"Altropane, a SPECT or PET Imaging Probe for Dopamine Neurons:
II. Distribution to Dopamine-Rich Regions of Primate Brain", B.
K. Madras, L. M. Gracz, P. C. Meltzer, A.Y. Liang, D. R. Elmaleh, M.
J. Kaufman, and A. J. Fischman, Synapse, 29, 105-115, 1998.
"Altropane, a SPECT or PET Imaging Probe for Dopamine Neurons:
III. Human Dopamine Transporter in Postmortem Normal and Parkinson's
Diseased Brain", B. K. Madras, L. M. Gracz, M. A. Fahey, D. R.
Elmaleh, P. C. Meltzer, A Y. Liang, E. G. Stopa, J. W. Babich, and A.
J. Fischman, Synapse, 29, 116-127, 1998.
"Structure Activity Relationships of Inhibition of the Dopamine
Transporter by 3-Arylbicyclo[3.2.1] octanes", P. C. Meltzer, P.
Blundell, and B. K. Madras, Med. Chem. Res., 8, 12-34, 1998.
1997
"Synthesis and Pharmacology of (R)- and-(S)-4'-Hydroxy-Δ8-Tetrahydrocanabinnols
(THCs)", Singer, M.; Dutta, A. K.; Compton, D. R.; Martin, B. R.;
Razdan, R. K. Eur. J. Med. Chem. 1997, 32, 165.
"Synthesis, Pharmacology and Molecular Modeling of Novel 4-Alkyloxy
Indole Derivatives Related to Cannabimimetic Aminoalkyl Indoles (AAIs)",
Dutta, A. K.; Ryan, W.; Thomas, B. F.; Singer, M.; Compton, D. R.; Martin,
B. R.; Razdan, R. K. Bioorg. Med. Chem. 1997, 5, 1591.
"Potent Anandamide Analogs: The Effect of Changing the Length
and Branching of the End Pentyl Chain", Ryan, W. J.; Banner, W.
K.; Wiley, J. L.; Martin, B. R.; Razdan, R. K. J. Med. Chem. 1997, 40,
3617.
"Evaluation of Cannabimimetic Discriminative Stimulus Effects
of Anandamide and Methylated Fluoroanandamide in Rhesus Monkeys",
Wiley, J. L.; Golden, K. M.; Ryan, W. J.; Balster, R. L.; Razdan, R.
K.; Martin, B. R. Pharmacol. Biochem. Behav. 1997,58, 1139.
"Synthesis of (+)- and (-)-2-Methylarachidonyl-2'-Fluoroethylamide
(O-689)", Ryan, W. J.; Banner, W. K.; Crocker, P. C.; Martin, B.
R.; Razdan, R. K. Bioorg. Med. Chem. Lett. 1997, 7, 2669.
"SPECT imaging of dopamine transporter sites in normal and MPTP-treated
rhesus monkeys", A. J. Fischman, J. W. Babich, D. R. Elmaleh, S.
A Barrow, P. C. Meltzer, R. N. Hanson, B. K. Madras, J. Nucl. Med. 38,
1997, 144-150.
"SPECT imaging of the dopamine transporter with [123I]-2β-carbomethoxy-3β-(4-fluorophenyl)-N-(1-iodoprop-1en-3-yl)nortropane
([123I]IACFT): initial experience in humans", A. J. Fischman, A.
A. Bonab, J. W. Babich, N. A. Alpert, D. R. Elmaleh, S. A Barrow, W.
Graham, P. C. Meltzer, R. N. Hanson, B. K. Madras, Neuroscience-Net,
1, #00010, 1997.
"Synthesis of 6- or 7- hydroxy and 6- or 7- methoxy tropanes",
Z. Chen, P. C. Meltzer, Tet. Lett. 1997, 38, 1121-1124.
"A 99mTechnetium SPECT imaging agents which targets the dopamine
transporter in primate brain", P. C. Meltzer, P. Blundell, A. G.
Jones, A. Mahmood, B. Garada, R. E Zimmerman, A. Davison, B. L. Holman,
B. K. Madras, J. Med. Chem., 40, 1835-1844, 1997.
"2-Carbomethoxy-3-aryl-8-oxabicyclo[3.2.1]octanes: Potent Non-Nitrogen
Inhibitors of Monoamine Transporters", P. C. Meltzer, A. Y. Liang,
P. Blundell, M. D. Gonzalez, Z. Chen, C. George, and B. K. Madras, J.
Med. Chem., 40, 2661-2673, 1997.
" A Ring Opening Rearrangement Reaction of 6b-Hydroxtropinone",
Z. Chen, M. D. Gonzalez, P. Blundell, P. C. Meltzer, Tet. Lett., 38,
6823-6824, 1997.
1996
"Structure-Activity Analysis of Anandamide Analogs: Relationship
to a Cannabinoid Pharmacophore", Thomas, B. F.; Adams, I. B.; Mascarella,
S. W.; Martin, B. R.; Razdan, R. K. J. Med. Chem. 1996, 39, 471.
"Agonist-antagonist characterization of 6'-cyanohex-2'-yne-Δ8-tetrahydrocannabinol
in two isolated tissue preparations", Pertwee, R. G.; Fernando,
S. R.; Griffin, G.; Ryan, W.; Razdan, R. K.; Compton, D. R.; Martin,
B. R. Eur. J. Pharmacol. 1996, 315, 195.
"Evaluation of Agonist-Antagonist Properties of Nitrogen Mustard
and Cyano Derivatives of Δ8-Tetrahydrocannabinol", Wiley, J. L.;
Compton, D. R.; Gordon, P. M.; Siegel, C.; Singer, M.; Dutta, A. K.;
Lichtman, A. H.; Balster, R. L.; Razdan, R. K.; Martin, B. R. Neuropharmacol.
1996, 35, 1793.
"2-Carbomethoxy-3-(diarylmethoxy)-1aH,5aH-tropane analogs: Synthesis
and inhibition of binding at the dopamine transporter and comparison
with piperazines of the GBR series", P. C. Meltzer, A. Y. Liang,
B. K. Madras, J. Med. Chem., 39, 371-379, 1996.
"Technepine: A high-affinity 99mTechnetium probe to label the
dopamine transporter in brain by SPECT imaging", B. K. Madras,
A. G. Jones, A. Mahmood, R. E. Zimmerman, B. Garada, B. L. Holman, A.
Davison, P. Blundell, P. C. Meltzer, Synapse, 22, 239-246, 1996.
"Design and synthesis of technepine: A 99mTechnetium probe which
labels the dopamine transporter", P. C. Meltzer, P. Blundell, A.
G. Jones, A. Mahmood, R. E. Zimmerman, B. Garada, B. L. Holman, A. Davison,
B. K. Madras, CPDD, abstract, 1996
" Nitrogen-based drugs are not essential for blockade of monoamine
transporters", B. K. Madras, Z. B. Pristupa, H. B. Niznik, A. Y.
Liang, P. Blundell, M. D. Gonzalez, P. C. Meltzer, Synapse, 24, 340-348,
1996.
"Preparation and biological evaluation of iodine-125-IACFT:
A selective SPECT agent for imaging dopamine transporter sites",
D. R. Elmaleh, A. J. Fischman, T. M. Shoup, B. Chang, R. N. Hanson,
A. Y. Liang, P. C. Meltzer, B. K. Madras, J. Nucl. Med. 37, 1197-1202,
1996.
"Cocaine congeners as PET imaging probes for dopamine terminals",
A-L. Brownell, D. R. Elmaleh, P. C. Meltzer, T. M. Shoup, G. L. Brownell,
A. J. Fischman, B. K. Madras, J. Nucl. Med. 37, 1186-1192, 1996.
1995
"Evaluation of Cannabinoid Receptor Binding and in vivo Activities
of Anandamide Analogs", I.B. Adams, W. Ryan, M. Singer, B.F. Thomas,
D.R. Compton, R.K. Razdan, B.R. Martin, J. Pharmacol. Exp. Ther. 1995,
273, 1172.
"A Novel Class of Potent Tetrahydrocannabinols (THCs): 2'-yne-Δ8-
and Δ9-THCs", W. Ryan, M. Singer, R.K. Razdan, D.R. Compton, B.R.
Martin, Life Sci. 1995, 56, 2013.
"Pharmacological And Behavioral Evaluation Of Alkylated Anandamide
Analogs", Adams, I. B.; Ryan, W.; Singer, M.; Razdan, R.K.; Compton,
D. R.; Martin, B. R. Life Sci. 1995, 56, 2041.
"Pharmacological Evaluation of Dimethylheptyl Analogs of Δ9-THC:
Reassessment of the Putative Three Point Cannabinoid-Receptor Interaction",
Martin, B. R.; Compton, D. R.; Prescott, W. R.; Barret, R. L.; Razdan,
R. K. Drug and Alcohol Dependence 1995, 37, 231.
"Characterization of Anandamide and Fluoroanandamide induced
Antinociception and Cross Tolerance to Δ9-THC after Intrathecal Administration
to Mice: Blockade of Δ9-THC-induced Antinociception", Welch, S.
P.; Dunlow, L. D.; Patrick, G. S.; Razdan, R. K. J. Pharmacol. Exp.
Ther. 1995, 273, 1235.
"The Synthesis and Pharmacological Evaluation of the Cannabinoid
Antagonist SR14176A", Dutta, A. K.; Sard, H.; Ryan, W.; Razdan,
R. K.; Compton, D. R.; Martin, B. R. Med. Chem.Res. 1995, 5, 54.
"Cyclization of 3-Fluorophenol and 3,3-Dimethylacrylic acid:
A Structure Correction" F. Shawcross and H. Sard J. Het. Chem.,
32, 1393, 1995.
"Encyclopedia of Reagents for Organic Synthesis", H. Sard,
contributor; L. Paquette, Editor, John Wiley and Sons, Ltd., Sussex,
UK, 1995.
"Difluoropine. A highly selective cocaine analog for PET studies
of dopamine transporters: Preliminary evaluation in the monkey brain",
B. K. Madras, D. R. Elmaleh, P. C. Meltzer, A. Y.Liang, T. Shoup, A.
J. Fischman, and A-L. Brownell, J. Nucl. Chem.,36, 117, 1995.
"I-123 IACFT: Radiolabeling and biodistribution in rats",
J. W. Babich, P. C. Meltzer, W. Graham, D. R. Elmaleh, B. K. Madras,
and A. J. Fischman, J. Nucl. Chem., 36, 145, 1995.
"SPECT imaging of dopamine transporter sites in normal and MPTP
treated Rhesus monkeys", A. J. Fischman, J. W. Babich, D. R. Elmaleh,
P. C. Meltzer, S. A. Barrow, and B. K. Madras, J. Nucl. Chem., 36, 87,
1995.
"Peptide Nucleic Acids: Synthesis of Thymine, Adenine, Guanine
and Cytosine Nucleobases", P. C. Meltzer, A. Liang, and P. Matsudaira,
J. Org. Chem, 60, 4305-4308, 1995.
"Altropane: A novel SPECT imaging agent for cocaine binding
sites on the dopamine transporter", B. K. Madras, L. M. Gracz,
M. J. Kaufman, P. C. Meltzer, D. Elmaleh, A. J. Fischman, CPDD, abstract
, 1995
" SAR of difluoropine: A potent and selective ligand for the
dopamine transporter", P. C. Meltzer, A. Y. Liang, and B. K. Madras,
CPDD, abstract, 1995
1994
"The Pharmacological Activity of Anandamide, A Putative Endogenous
Cannabinoid, in Mice", P.B. Smith, D.R. Compton, S.P. Welch, R.K.
Razdan, R. Mechoulam, and B.R. Martin, J. Pharmacol. Exper. Ther. 1994,270,
219.
"Synthesis of (R)- and (S)-4'-Acetoxyolivetol [5-(4-acetoxypentyl)-1,3-benzenediol]:
Key Intermediates in the Synthesis of tetrahydrocannabinol Derivatives",
M. Singer, C. Siegel, P.M. Gordon, A.K. Dutta, R.K. Razdan, Synthesis
1994, 486.
"An Unexpected Product During Synthesis of 3-Phenylisoquinoline:
Improved Preparation of 4-Hydroxy-3-phenylisoquinoline" H. Sard,
J. Het. Chem. 31, 1085, 1994.
"Synthesis and Antiviral Activity of the Cyclopropano Homolog
of 2,3-Didehydro-2,3-dideoxythymidine" H. Sard, Nucleosides and
Nucleotides 13, 2321, 1994.
"The Discovery of an Unusually Selective and Novel Cocaine Analog:
Difluoropine. Synthesis and Inhibition of Binding at Cocaine Recognition
Sites", P. C. Meltzer, A. Liang, and B. K. Madras, J. Med. Chem.,
37, 2001-2010, 1994.
"O-526, a piperidine analog of GBR 12909, retains high affinity
for the dopamine transporter in monkey caudate-putamen", B. K.
Madras, M.E.A. Reith, P. C. Meltzer, and A. K Dutta, Eur. J. Pharmacol.,
267, 167-173, 1994.
"Positron Emission Tomography of cocaine Bonding Sites on the
Dopamine Transporter", B.K. Madras, D. E. Elmaleh, P. C. Meltzer,
A. Y. Liang, G. L. Brownell, and A-L. Brownell, NIDA Res. Mono., 138,
57- 68, 1994.
"In contrast to R-cocaine/R-cocaine analogs, novel S-analogs
of benztropine are potent and selective inhibitors of the dopamine transporter:
implications for cocaine binding", B. K. Madras, A. Liang, and
P. C. Meltzer, CPDD, abstract 112, 1994.
"The Discovery of a Novel Tropane Analog which binds Potently
and Selectively to the Dopamine Transporter", P. C. Meltzer, A.
Liang, and B. K. Madras, CPDD, abstract 111, 1994.
"Pet imaging of cocaine binding sites on the dopamine transporter:
An application for medications development", A-L. Brownell, D.
E. Elmaleh, P. C. Meltzer, and B. K. Madras, CPDD, abstract 121, 1994.
"In contrast to inactive S-cocaine, a novel series of S-cocaine
congeners display high affinity and selectivity for the dopamine transporter",
B. K. Madras, A. Liang, and P. C. Meltzer. Society for Neuroscience,
abstract, 1994.
1993
"Cannabinoid Structure-Activity Relationships: Correlation of
Receptor Binding and in vivo Activities" D.R. Compton, K.C. Rice,
B.R. Decosta, R.K. Razdan, L.S. Melvin, M.R. Johnson and B.R. Maring,
J. Pharmacol. Exper. Ther. 1993, 265, 218.
"Substituted 3-Phenyltropane Analogs of Cocaine: Synthesis and
Inhibition of Binding at the Cocaine Receptor", P. C. Meltzer,
A. Liang, A. L. Brownell, D. R. Elmaleh, and B. K. Madras, J. Med. Chem.,
36, 855-862, 1993.
"High Affinity Probes for Cocaine Recognition Sites on the Dopamine
Transporter", L. M. Gracz, B. K. Madras, R. Hanson, D. Elmaleh,
P. C. Meltzer, Society for Neuroscience Abstracts, #617.6, 19, 1993.
"Positional Importance of the Nitrogen Atom in Novel Piperidine
Analogs of GBR 12909: Affinity and Selectivity for the Dopamine Transporter",
A. K. Dutta, P. C. Meltzer, and B. K. Madras, Med. Chem. Res., 3, 209-222,
1993.
1992
"Cocaine Congeners as Probes for Cocaine Receptors and Parkinson's
Disease", B. Madras, D. R. Elmaleh, P. C. Meltzer, A. Liang, G.
Brownell, and A. L. Brownell, American Nuclear Society, 65, 8-9, 1992.
"PET Imaging Probes for the Cocaine Receptors: A Validation
Study in a Nonhuman Primate Model", D. R. Elmaleh, P. C. Meltzer,
B. K. Madras, A. Liang, A. L. Brownell, P. Hantraye, O. Isacson, T.
Shoup, A. J. Fischman, G. L. Brownell, and H. W. Strauss, Presentation
at the Society for Nuclear Medicine, 39th Annual Meeting, Los Angeles,
June, 1992.
"Synthesis and C-11 Labeling of some 3β-Phenyltropane-2-carboxylic
esters (WIN) Analogs for PET", D. R. Elmaleh, P. C. Meltzer, B.
Madras, A. Liang, A. L. Brownell, P. Hantraye, O. Isacson, T. Shoup,
A. J. Fischman, G. L. Brownell, and H. W. Strauss, Presentation at the
International Symposium Radiopharmaceutical Chemistry, Paris, France,
1992.
"Halogenated Cocaine Analogs: Lack of Correlation between Ligand
Binding Affinity, In Vivo Potency, and In Vivo Efficacy", David
R. Compton and Peter C. Meltzer, Presentation at ASPET, Orlando, Florida,
1992.
"The Dopamine transporter: a target of cocaine-like drugs and
a marker for Parkinson's disease", B. K. Madras, M. J. Kaufman,
M.A. Fahey, S. Kish, K. Shannak, O. Hornykiewicz, P. C. Meltzer, P.
Hantraye, G. L. Brownell, D. R. Elmaleh, A. L. Brownell, 7th International
Catechol Symposium, 193, 1992.
"Parkinsonian Signs in MPTP-treated Monkeys are Alleviated by
the High Efficacy D1 Dopamine Receptor Agonist SKF 81297", B. K.
Madras, D. R. Elmaleh, P. C. Meltzer, D. E. Lee-Parritz, P. Hantraye,
O. Isacson, G. L. Brownell, and A. L. Brownell, Society for Neuroscience
Abstracts, #935, 18, 1992.
1991
"An Expedient and Efficient Synthesis of an Optically Active
Terpene Synthon for Δ9-Cannabinoids", P.M. Gordon, C. Siegel and
R.K. Razdan, Chem. Commun. 1991, 692.
"Studies on the synthesis of (-)-11-Nor-9-carboxy-Δ9-tetrahydrocannabinol
(THC) and related compounds: An Improved Oxidative Procedure",
C. Siegel, P.M. Gordon, and R.K. Razdan, Synthesis 1991, 851.
"Behavioral, Biochemical and Molecular Modeling Evaluations
of Cannabinoid Analogs", B.R. Martin, D.R. Compton, B.F. Thomas,
W.R. Prescott, P.J. Little, R.K. Razdan, M.R. Johnson, L.S. Melvin,
R. Mechoulam and S.J. Ward, Pharmacol. Biochem. Behav. 1991, 40, 471.
"Synthesis of Racemic and Optically Active Δ9-Tetrahydrocannabinol
(THC) Metabolites", C. Siegel, P.M. Gordon, D.B. Uliss, G.R. Handrick,
H.C. Dalzell and R.K. Razdan, J. Org. Chem. 1991, 56, 6865.
"Synthesis and Pharmacological Evaluation of Ether and Related
Analogues of Δ8, Δ9-, and Δ9, 11-Tetrahydrocannabinol", D.R. Compton,
W.R. Prescott Jr., B.R. Martin, C. Siegel, P.M. Gordon and R.K. Razdan,
J. Med. Chem. 1991, 34, 3310.
"Imaging Probes for Cocaine Receptors in Human and Nonhuman
Primate Brain", B. Madras, M. J. Kaufman, R. D. Spealman, M. A.
Fahey, P. C. Meltzer, A. Liang, A-L. Brownell, J. Schumacher, O. Isacson,
G. L. Brownell, and D. R. Elmaleh, Problems of Drug Dependence, 1991,
Proc. of the 53rd Annual Scientific Meeting, CPDD.
1990
"Synthesis and Pharmacological Evaluation of Amino, Azido, and
Nitrogen Mustard Analogues of 10-substituted cannabidiol and 11- or
12- substituted Δ8-Tetrahydrocannabinol", D.R. Compton, P.J. Little,
B.R. Martin, J.W. Gilman, J.K. Saha, V.S. Jorapur, H.P. Sard and R.K.
Razdan, J. Med. Chem. 1990, 33, 1437.
1989
"Synthesis and Pharmacological evaluation of mercapto and thioacetyl
analogues of cannabidiol and Δ8-tetrahydrocannabinol", D.R. Compton,
P.J. Little, B.R. Martin, J.K. Saha, J. Gilman, H. Sard and R.K. Razdan,
Eur. J. Med. Chem. 1989, 24, 293.
"An optically Active Terpenic Synthon for Δ9-cannabinoids: Synthesis
of (-)-11-Hydroxy-Δ9-tetrahydrocannabinol (THC) and its 1',1'-Dimethylheptyl
Analogue", C. Siegel, P.M. Gordon and R.K. Razdan, J. Org. Chem.
1989, 54, 5428.
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