TY - JOUR
T1 - 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
AU - Kumar Srivastava, Brijesh
AU - Soni, Rina
AU - Patel, Jayendra Z.
AU - Jha, Satadru
AU - Shedage, Sandeep A.
AU - Gandhi, Neha
AU - Sairam, Kalapatapu V.V.M.
AU - Pawar, Vishwanath
AU - Sadhwani, Nisha
AU - Mitra, Prasenjit
AU - Jain, Mukul R.
AU - Patel, Pankaj R.
PY - 2008/7/15
Y1 - 2008/7/15
N2 - 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.
AB - 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.
UR - https://www.scopus.com/pages/publications/48949115102
UR - https://www.scopus.com/pages/publications/48949115102#tab=citedBy
U2 - 10.1016/j.bmcl.2008.06.045
DO - 10.1016/j.bmcl.2008.06.045
M3 - Article
C2 - 18585913
AN - SCOPUS:48949115102
SN - 0960-894X
VL - 18
SP - 3882
EP - 3886
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 14
ER -