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
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 aminopiperid...
| Main Authors: | , , , , , , , , , , , |
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| Format: | Journal Article |
| Published: |
Pergamon
2008
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| Online Access: | http://hdl.handle.net/20.500.11937/27282 |
| _version_ | 1848752220206530560 |
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| author | 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. |
| author_facet | 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. |
| author_sort | Kumar Srivastava, B. |
| building | Curtin Institutional Repository |
| collection | Online Access |
| description | 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. |
| first_indexed | 2025-11-14T08:05:09Z |
| format | Journal Article |
| id | curtin-20.500.11937-27282 |
| institution | Curtin University Malaysia |
| institution_category | Local University |
| last_indexed | 2025-11-14T08:05:09Z |
| publishDate | 2008 |
| publisher | Pergamon |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | curtin-20.500.11937-272822017-09-13T15:33:15Z 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. 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. 2008 Journal Article http://hdl.handle.net/20.500.11937/27282 10.1016/j.bmcl.2008.06.045 Pergamon restricted |
| spellingShingle | 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. 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 |
| title | 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 |
| title_full | 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 |
| title_fullStr | 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 |
| title_full_unstemmed | 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 |
| title_short | 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 |
| title_sort | 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 |
| url | http://hdl.handle.net/20.500.11937/27282 |