Discovery of novel, orally available benzimidazoles as melanin concentrating hormone receptor 1 (MCHR1) antagonists.

Abstract

Melanin concentrating hormone (MCH) is an important mediator of energy homeostasis and plays role in several disorders such as obesity, stress, depression and anxiety. The synthesis and biological evaluation of novel benzimidazole derivatives as MCHR1 antagonists are described. The in vivo proof of principle for weight loss with a lead compound from this series is exemplified.

• Authors: Pradip K Sasmal, Sanjita Sasmal, P Tirumala Rao, B Venkatesham, M Roshaiah, Chandrasekhar Abbineni, Ish Khanna, Vikram P Jadhav, J Suresh, Rashmi Talwar, Syed Muzeeb, Jean-Marie Receveur, Thomas M Frimurer, Øystein Rist, Lisbeth Elster, Thomas Högberg
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 20 Issue 18 Pg. 5443-8 (Sep 15 2010) ISSN: 1464-3405 [Electronic] England
• PMID: 20724156 (Publication Type: Journal Article)
• Copyright: Copyright (c) 2010 Elsevier Ltd. All rights reserved.

Chemical References

• Anti-Obesity Agents
• Benzimidazoles
• MCHR1 protein, human
• Receptors, Somatostatin

Topics

• Animals
• Anti-Obesity Agents (chemical synthesis, chemistry, pharmacology, therapeutic use)
• Benzimidazoles (chemical synthesis, chemistry, pharmacology, therapeutic use)
• Humans
• Mice
• Mice, Inbred C57BL
• Models, Molecular
• Obesity (drug therapy)
• Protein Binding
• Receptors, Somatostatin (antagonists & inhibitors, metabolism)
• Weight Loss (drug effects)