Facile synthesis, ex-vivo and in vitro screening of 3-sulfonamide derivative of 5-(4-chlorophenyl)-1
July 3rd, 2008 | by admin |Facile synthesis, ex-vivo and in vitro screening of 3-sulfonamide derivative of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide (SR141716) a potent CB1 receptor antagonist.
Facile synthesis of biaryl pyrazole sulfonamide derivative of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide (SR141716, 1) and an investigation of the effect of replacement of the -CO group in the compound 1 by the -SO(2) group in the aminopiperidine region is reported. Primary ex-vivo pharmacological testing and in vitro screening of sulfonamide derivative 2 showed the loss of CB1 receptor antagonism.
Kumar Srivastava B, Soni R, Patel JZ, Jha S, Shedage SA, Gandhi N, Sairam KV, Pawar V, Sadhwani N, Mitra P, Jain MR, Patel PR.
Department of Medicinal Chemistry, Zydus Research Centre, Cadila Healthcare Ltd., Sarkhej-Bavla N. H.8A, Moraiya, Ahmedabad 382210, India.