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

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. (2008) 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. Bioorganic & Medicinal Chemistry Letters, 18(14), pp. 3882-3886.

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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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ID Code: 93837
Item Type: Journal Article
Refereed: Yes
DOI: 10.1016/j.bmcl.2008.06.045
ISSN: 0960-894X
Deposited On: 04 Apr 2016 06:16
Last Modified: 19 Apr 2016 04:05

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