Synthesis, Biological Properties, and Molecular Modeling Investigations of Novel 3,4-Diarylpyrazolines as Potent and Selective CB<sub>1</sub> Cannabinoid Receptor Antagonists

H.M. Lange, Jos; K. A. C. Coolen, Hein; H. van Stuivenberg, Herman; Adriana Rigtje Dijksman, Jessica; H. J. Herremans, Arnoud; Ronken, Eric; G. Keizer, Hiskias; Tipker, Koos; C. McCreary, Andrew; Veerman, Willem; C. Wals, Henri; Stork, Bob; C. Verveer, Peter; P. den Hartog, Arnold; M. J. de Jong, Natasja; J. P. Adolfs, Tiny; Hoogendoorn, Jan; G. Kruse, Chris

doi:10.1021/jm031019q

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Synthesis, Biological Properties, and Molecular Modeling Investigations of Novel 3,4-Diarylpyrazolines as Potent and Selective CB1 Cannabinoid Receptor Antagonists

Published in Journal of Medicinal Chemistry • Dec 30, 2003

Authors:

Jos H.M. Lange

Hein K. A. C. Coolen

Herman H. van Stuivenberg

Abstract

A series of novel 3,4-diarylpyrazolines was synthesized and evaluated in cannabinoid (hCB(1) and hCB(2)) receptor assays. The 3,4-diarylpyrazolines elicited potent in vitro CB(1) antagonistic activities and in general exhibited high CB(1) vs CB(2) receptor subtype selectivities. Some key representat...

Subject

Chemistry

Intramolecular force

Rimonabant

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