Sasmal, Pradip K. ; Talwar, Rashmi ; Swetha, J. ; Balasubrahmanyam, D. ; Venkatesham, B. ; Rawoof, Khaji Abdul ; Neelima Devi, B. ; Jadhav, Vikram P. ; Khan, Sanjoy K. ; Mohan, Priya ; Srinivasa Reddy, D. ; Nyavanandi, Vijay Kumar ; Nanduri, Srinivas ; Shiva Kumar, K. ; Kannan, M. ; Srinivas, P. ; Nadipalli, Prabhakar ; Chaudhury, Hira ; Sebastian, V.J. (2011) Structure–activity relationship studies of novel pyrazole and imidazole carboxamides as cannabinoid-1 (CB1) antagonists Bioorganic & Medicinal Chemistry Letters, 21 (16). pp. 4913-4918. ISSN 0960-894X
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Official URL: http://doi.org/10.1016/j.bmcl.2011.06.017
Related URL: http://dx.doi.org/10.1016/j.bmcl.2011.06.017
Abstract
The synthesis and biological evaluation of novel pyrazole and imidazole carboxamides as CB1 antagonists are described. As a part of eastern amide SAR, various chemically diverse motifs were introduced on rimonabant template. The central pyrazole core was also replaced with its conformationally constrained motif and imidazole moieties. In general, a range of modifications were well tolerated. Several molecules with low- and sub-nanomolar potencies were identified as potent CB1 receptor antagonists. The in vivo proof of principle for weight loss is demonstrated with a lead compound in DIO mice model.
| Item Type: | Article |
|---|---|
| Source: | Copyright of this article belongs to National Library of Medicine |
| ID Code: | 122004 |
| Deposited On: | 27 Jul 2021 09:02 |
| Last Modified: | 30 Jul 2021 12:40 |
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