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

被引：27

作者：

Sasmal, Pradip K. ^{[1
]}

Reddy, D. Srinivasa ^{[1
]}

Talwar, Rashmi ^{[1
]}

Venkatesham, B. ^{[1
]}

Balasubrahmanyam, D. ^{[1
]}

Kannan, M. ^{[1
]}

Srinivas, P. ^{[1
]}

Kyasa, Shiva K. ^{[1
]}

Devi, B. Neelima ^{[1
]}

Jadhav, Vikram P. ^{[1
]}

Khan, Sanjoy K. ^{[1
]}

Mohan, Priya ^{[1
]}

Chaudhury, Hira ^{[1
]}

Bhuniya, Debnath ^{[1
]}

Iqbal, Javed ^{[1
]}

Chakrabarti, Ranjan ^{[1
]}

机构：

[1] Dr Reddys Labs Ltd, Discovery Res, Hyderabad 500049, Andhra Pradesh, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 01期

关键词：

Cannabinoid-1 (CB1) receptor; CB1; antagonists; Pyrazole-3-carboxamides; Obesity; DIO mice model; RECEPTOR INVERSE AGONIST; ENDOCANNABINOID SYSTEM; BODY-WEIGHT; FOOD-INTAKE; POTENT; RIMONABANT; TARANABANT; DISCOVERY; MK-0364; ADIPOSE;

D O I：

10.1016/j.bmcl.2010.10.055

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：562 / 568

页数：7

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