2. Academic Validation
  3. Structure-activity relationship studies of novel pyrazole and imidazole carboxamides as cannabinoid-1 (CB1) antagonists

Structure-activity relationship studies of novel pyrazole and imidazole carboxamides as cannabinoid-1 (CB1) antagonists

  • Bioorg Med Chem Lett. 2011 Aug 15;21(16):4913-8. doi: 10.1016/j.bmcl.2011.06.017.
Pradip K Sasmal 1,  Rashmi Talwar,  J Swetha,  D Balasubrahmanyam,  B Venkatesham,  Khaji Abdul Rawoof,  B Neelima Devi,  Vikram P Jadhav,  Sanjoy K Khan,  Priya Mohan,  D Srinivasa Reddy,  Vijay Kumar Nyavanandi,  Srinivas Nanduri,  Shiva K Kyasa,  M Kannan,  P Srinivas,  Prabhakar Nadipalli,  Hira Chaudhury,  V J Sebastian
Affiliations

Affiliation

  • 1 Discovery Research, Dr. Reddy's Laboratories Ltd, Bollaram Road, Miyapur, Hyderabad 500049, India. sasmalpk@yahoo.co.in
PMID: 21741835 DOI: 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.

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