Novel pyrazole-3-carboxamide derivatives as cannabinoid-1 (CB1) antagonists: Journey from non-polar to polar amides

作者：Sasmal Pradip K^*; Reddy D Srinivasa; Talwar Rashmi; Venkatesham B; Balasubrahmanyam D; Kannan M; Srinivas P; Kumar K Shiva; Devi B Neelima; Jadhav Vikram P; Khan Sanjoy K; Mohan Priya; Chaudhury Hira; Bhuniya Debnath; Iqbal Javed; Chakrabarti Ranjan

来源：Bioorganic & Medicinal Chemistry Letters, 2011, 21(1): 562-568.

DOI：10.1016/j.bmcl.2010.10.055

• Cannabinoid-1 (CB1) receptor
• CB1 antagonists
• Pyrazole-3-carboxamides
• Obesity
• DIO mice model

The synthesis and biological evaluation of novel pyrazole-3-carboxamide derivatives as CB1 antagonists are described. As a part of eastern amide SAR, various chemically diverse motifs were introduced. In general, a range of modifications were well tolerated. Several molecules with high polar surface area were also indentified as potent CB1 receptor antagonists. The in vivo proof of principle for weight loss is exemplified with a lead compound from this series.

• 出版日期2011-1