Chemical and biological investigation of cyclopropyl containing diaryl-pyrazole-3-carboxamides as novel and potent cannabinoid type 1 receptor antagonists

…, A Szemzo, P Erdélyi, K Vukics, J Szikra…

Index: Szabo, Gyorgy; Varga, Balazs; Payer-Lengyel, Dora; Szemzo, Attila; Erdelyi, Peter; Vukics, Krisztina; Szikra, Judit; Hegyi, Eva; Vastag, Monika; Kiss, Bela; Laszy, Judit; Gyertyan, Istvan; Fischer, Janos Journal of Medicinal Chemistry, 2009 , vol. 52, # 14 p. 4329 - 4337

Full Text: HTML

Citation Number: 26

Abstract

Obesity is a major clinical problem in the western world, and many molecular targets have been explored in the search for effective therapeutic agents. One of these, antagonism of the cannabinoid 1 (CB1) receptor, rose to prominence following reports demonstrating the positive modulation of food intake by the CB1 antagonist, rimonabant (3)(SR141716A). In the present study, various diaryl-pyrazole derivatives containing cycloalkyl building blocks ...