Title of article :
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
Author/Authors :
Brijesh Kumar Srivastava، نويسنده , , Rina Soni، نويسنده , , Jayendra Z. Patel، نويسنده , , Satadru Jha، نويسنده , , Sandeep A. Shedage، نويسنده , , Neha Gandhi، نويسنده , , Kalapatapu V.V.M. Sairam، نويسنده , , Vishwanath Pawar، نويسنده , , Nisha Sadhwani، نويسنده , , Prasenjit Mitra، نويسنده , , Mukul R. Jain، نويسنده , , Pankaj R. Patel، نويسنده ,
Abstract :
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 –SO2 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.
Keywords :
hCB1(cAMP)assay , Mouse vas defense assay , Sulfonamide derivative , CB1 receptor antagonist , PLP (piece-wise linear potential) scores
