Synthesis, cannabinoid receptor affinity, and molecular modeling studies of substituted 1-aryl-5-(1 H-pyrrol-1-yl)-1 H-pyrazole-3-carboxamides

…, A Brizzi, S Pasquini, M Botta, E Novellino…

Index: Silvestri, Romano; Cascio, Maria Grazia; La Regina, Giuseppe; Piscitelli, Francesco; Lavecchia, Antonio; Brizzi, Antonella; Pasquini, Serena; Botta, Maurizio; Novellino, Ettore; Di Marzo, Vincenzo; Corelli, Federico Journal of Medicinal Chemistry, 2008 , vol. 51, # 6 p. 1560 - 1576

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Citation Number: 57

Abstract

The new 1-phenyl-5-(1 H-pyrrol-1-yl) pyrazole-3-carboxamides were compared with the reference compounds AM251 and SR144528 for cannabinoid hCB1 and hCB2 receptor affinity. Compounds bearing 2, 4-dichlorophenyl or 2, 4-difluorophenyl groups at position 1 and 2, 5-dimethylpyrrole moiety at position 5 of the pyrazole nucleus were generally more selective for hCB1. On the other hand, the N-cyclohexyl group at the 3-carboxamide was ...