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

Autoria(s): 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.
Data(s)

2008
Resumo

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.
Identificador

http://eprints.qut.edu.au/93837/
Publicador

Elsevier
Relação

DOI:10.1016/j.bmcl.2008.06.045

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.
Tipo

Journal Article
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