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-carboxy lic acid piperidin-1-ylamide (SR141716) a potent CB1 receptor antagonist

Kumar Srivastava, B.; Soni, R.; Patel, J.; Jha, S.; Shedage, S.; Gandhi, Neha; Sairam, K.; Pawar, V.; Sadhwani, N.; Mitra, P.; Jain, M.; Patel, P.

doi:10.1016/j.bmcl.2008.06.045

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Authors

Kumar Srivastava, B.

Soni, R.

Patel, J.

Jha, S.

Shedage, S.

Gandhi, Neha

Sairam, K.

Pawar, V.

Sadhwani, N.

Mitra, P.

Jain, M.

Patel, P.

Date

2008

Type

Journal Article

Metadata

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Citation

Kumar Srivastava, B. and Soni, R. and Patel, J. and Jha, S. and Shedage, S. and Gandhi, N. and Sairam, K. et al. 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-carboxy lic acid piperidin-1-ylamide (SR141716) a potent CB1 receptor antagonist. Bioorganic & Medicinal Chemistry Letters. 18 (14): pp. 3882-3886.

Source Title

Bioorganic & Medicinal Chemistry Letters

DOI

10.1016/j.bmcl.2008.06.045

ISSN

0960-894X

School

School of Biomedical Sciences

URI

http://hdl.handle.net/20.500.11937/27282

Collection

Curtin Research Publications

Abstract

Facile synthesis of biaryl pyrazole sulfonamide derivative of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxy lic 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. © 2008 Elsevier Ltd. All rights reserved.