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 |
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| Authors: | Kumar Srivastava Brijesh Soni Rina Patel Jayendra Z Jha Satadru Shedage Sandeep A Gandhi Neha Sairam Kalapatapu V V M Pawar Vishwanath Sadhwani Nisha Mitra Prasenjit Jain Mukul R Patel Pankaj R |
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| Institution: | Department of Medicinal Chemistry, Zydus Research Centre, Cadila Healthcare Ltd., Sarkhej-Bavla N. H.8A, Moraiya, Ahmedabad 382210, India. brijeshsrivastava@zyduscadila.com |
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| 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. |
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| Keywords: | Mouse vas defense assay Sulfonamide derivative CB1 receptor antagonist PLP (piece-wise linear potential) scores hCB1(cAMP)assay |
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