Bioisosteric Replacements of the Pyrazole Moiety of Rimonabant:  Synthesis, Biological Properties, and Molecular Modeling Investigations of Thiazoles, Triazoles, and Imidazoles as Potent and Selective CB<sub>1</sub>Cannabinoid Receptor Antagonists

H.M. Lange, Jos; H. van Stuivenberg, Herman; K. A. C. Coolen, Hein; J. P. Adolfs, Tiny; C. McCreary, Andrew; G. Keizer, Hiskias; C. Wals, Henri; Veerman, Willem; J. M. Borst, Alice; de Looff, Wouter; C. Verveer, Peter; G. Kruse, Chris

doi:10.1021/jm040843r

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Bioisosteric Replacements of the Pyrazole Moiety of Rimonabant: Synthesis, Biological Properties, and Molecular Modeling Investigations of Thiazoles, Triazoles, and Imidazoles as Potent and Selective CB1Cannabinoid Receptor Antagonists

Published in Journal of Medicinal Chemistry • Sep 29, 2004

Authors:

Jos H.M. Lange

Herman H. van Stuivenberg

Hein K. A. C. Coolen

Abstract

Series of thiazoles, triazoles, and imidazoles were designed as bioisosteres, based on the 1,5-diarylpyrazole motif that is present in the potent CB(1) receptor antagonist rimonabant (SR141716A, 1). A number of target compounds was synthesized and evaluated in cannabinoid (hCB(1) and hCB(2)) recepto...

Subject

Rimonabant

Chemistry

Pyrazole

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