Design, chemical synthesis, and biological evaluation of novel triazolyl analogues of taranabant (MK-0364), a cannabinoid-1 receptor inverse agonist

Tetrahedron ◽

10.1016/j.tet.2008.09.057 ◽

2008 ◽

Vol 64 (48) ◽

pp. 10802-10809 ◽

Author(s):

Min-ah Kim ◽

Hoseop Yun ◽

HyunJung Kwak ◽

Jeongmin Kim ◽

Jinhwa Lee

Keyword(s):

Chemical Synthesis ◽

Biological Evaluation ◽

Inverse Agonist ◽

Cannabinoid 1 Receptor ◽

Synthesis And Biological Evaluation ◽

Receptor Inverse Agonist

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Design, Synthesis, and Biological Evaluation of Retinoic Acid-Related Orphan Receptor γt (RORγt) Agonist Structure-Based Functionality Switching Approach from In House RORγt Inverse Agonist to RORγt Agonist

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.8b01181 ◽

2019 ◽

Vol 62 (3) ◽

pp. 1167-1179 ◽

Author(s):

Tomoya Yukawa ◽

Yoshi Nara ◽

Mitsunori Kono ◽

Ayumu Sato ◽

Tsuneo Oda ◽

...

Keyword(s):

Retinoic Acid ◽

Biological Evaluation ◽

Inverse Agonist ◽

Orphan Receptor ◽

Design Synthesis ◽

Synthesis And Biological Evaluation

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ChemInform Abstract: Overview of a Rational Approach to Design Type I 17β-Hydroxysteroid Dehydrogenase Inhibitors Without Estrogenic Activity: Chemical Synthesis and Biological Evaluation

10.1002/chin.199904257 ◽

2010 ◽

Vol 30 (4) ◽

pp. no-no

Author(s):

M. R. TREMBLAY ◽

D. POIRIER

Keyword(s):

Chemical Synthesis ◽

Estrogenic Activity ◽

Hydroxysteroid Dehydrogenase ◽

Biological Evaluation ◽

Rational Approach ◽

Type I ◽

Design Type ◽

Synthesis And Biological Evaluation

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Discovery of 2-[5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-1H-pyrazol-3-yl]-1,5,5-trimethyl-1,5-dihydro-imidazol-4-thione (BPR-890) via an Active Metabolite. A Novel, Potent and Selective Cannabinoid-1 Receptor Inverse Agonist with High Antiobesity Efficacy in DIO Mice

Journal of Medicinal Chemistry ◽

10.1021/jm900471u ◽

2009 ◽

Vol 52 (14) ◽

pp. 4496-4510 ◽

Author(s):

Chien-Huang Wu ◽

Ming-Shiu Hung ◽

Jen-Shin Song ◽

Teng-Kuang Yeh ◽

Ming-Chen Chou ◽

...

Keyword(s):

Active Metabolite ◽

Inverse Agonist ◽

Cannabinoid 1 Receptor ◽

Receptor Inverse Agonist

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In vitroandin vivometabolism of a novel cannabinoid-1 receptor inverse agonist, taranabant, in rats and monkeys

Xenobiotica ◽

10.3109/00498254.2010.501117 ◽

2010 ◽

Vol 40 (9) ◽

pp. 650-662 ◽

Author(s):

V.B.G. Reddy ◽

G.A. Doss ◽

B.V. Karanam ◽

K. Samuel ◽

T.J. Lanza Jr ◽

...

Keyword(s):

Inverse Agonist ◽

Cannabinoid 1 Receptor ◽

Receptor Inverse Agonist

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Chemical synthesis and biological evaluation of a NAD(P)H:quinone oxidoreductase-1 targeted tripartite quinone drug delivery system

Molecular Cancer Therapeutics ◽

10.1158/1535-7163.mct-07-0519 ◽

2007 ◽

Vol 6 (12) ◽

pp. 3122-3130 ◽

Author(s):

M. Volpato ◽

N. Abou-Zeid ◽

R. W. Tanner ◽

L. T. Glassbrook ◽

J. Taylor ◽

...

Keyword(s):

Drug Delivery ◽

Chemical Synthesis ◽

Drug Delivery System ◽

Delivery System ◽

Biological Evaluation ◽

Synthesis And Biological Evaluation

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Chemical Synthesis and Biological Evaluation of Second-Generation Palmerolide A Analogues

European Journal of Organic Chemistry ◽

10.1002/ejoc.201001562 ◽

2010 ◽

Vol 2011 (3) ◽

pp. 463-468 ◽

Author(s):

Vengala Rao Ravu ◽

Gulice Y. C. Leung ◽

Chek Shik Lim ◽

Sin Yee Ng ◽

Rong Ji Sum ◽

...

Keyword(s):

Chemical Synthesis ◽

Second Generation ◽

Biological Evaluation ◽

Palmerolide A ◽

Synthesis And Biological Evaluation

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Influence of taranabant, a cannabinoid-1 receptor inverse agonist, on pharmacokinetics and pharmacodynamics of warfarin

Advances in Therapy ◽

10.1007/s12325-008-0116-9 ◽

2008 ◽

Vol 25 (11) ◽

pp. 1175-1190 ◽

Author(s):

Jules I. Schwartz ◽

Stephanie Dunbar ◽

Jinyu Yuan ◽

Susie Li ◽

Adrianna Gipson ◽

...

Keyword(s):

Inverse Agonist ◽

Pharmacokinetics And Pharmacodynamics ◽

Cannabinoid 1 Receptor ◽

Receptor Inverse Agonist

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Conformational Analysis and Receptor Docking ofN-[(1S,2S)-3-(4-Chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-{[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (Taranabant, MK-0364), a Novel, Acyclic Cannabinoid-1 Receptor Inverse Agonist

Journal of Medicinal Chemistry ◽

10.1021/jm7014974 ◽

2008 ◽

Vol 51 (7) ◽

pp. 2108-2114 ◽

Author(s):

Linus S. Lin ◽

Sookhee Ha ◽

Richard G. Ball ◽

Nancy N. Tsou ◽

Laurie A. Castonguay ◽

...

Keyword(s):

Conformational Analysis ◽

Inverse Agonist ◽

Cannabinoid 1 Receptor ◽

Receptor Inverse Agonist

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Chemical synthesis and biological evaluation of novel epothilone B and trans-12,13-cyclopropyl epothilone B analogues

Tetrahedron ◽

10.1016/s0040-4020(02)00655-5 ◽

2002 ◽

Vol 58 (32) ◽

pp. 6413-6432 ◽

Author(s):

K.C Nicolaou ◽

Andreas Ritzén ◽

Kenji Namoto ◽

Rubén M Buey ◽

J.Fernando Dı́az ◽

...

Keyword(s):

Chemical Synthesis ◽

Biological Evaluation ◽

Epothilone B ◽

Synthesis And Biological Evaluation

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Molecular design, chemical synthesis, and biological evaluation of anthracene-carbohydrate hybrids as novel DNA photocleaving and photoselective cytotoxic agents

ARKIVOC ◽

10.3998/ark.5550190.0005.d04 ◽

2004 ◽

Vol 2004 (13) ◽

pp. 28-35 ◽

Author(s):

Kazunobu Toshima ◽

Masashi Hasegawa ◽

Junji Shimizu ◽

Shuichi Matsumura

Keyword(s):

Chemical Synthesis ◽

Molecular Design ◽

Biological Evaluation ◽

Cytotoxic Agents ◽

Synthesis And Biological Evaluation

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