Jump to main content
Jump to site search

Issue 5, 2011
Previous Article Next Article

Synthesis and SAR studies of benzimidazole derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists: Focus to detune hERG inhibition

Author affiliations

Abstract

Melanin concentrating hormone receptor 1 (MCHR1) antagonists are potentially useful in the treatment of several CNS disorders such as obesity, stress, depression and anxiety. In a previous article, we have described a novel series of benzimidazoles as MCHR1 antagonists. These compounds showed good efficacy in obesity models but the lead compound also showed potent inhibition of hERG potassium channel. Described herein the medicinal chemistry attempts to reduce hERG inhibition while retaining MCHR1 antagonistic profile.

Graphical abstract: Synthesis and SAR studies of benzimidazole derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists: Focus to detune hERG inhibition

Back to tab navigation

Publication details

The article was received on 18 Jan 2011, accepted on 06 Feb 2011 and first published on 07 Mar 2011


Article type: Concise Article
DOI: 10.1039/C1MD00015B
Med. Chem. Commun., 2011,2, 385-389

  •   Request permissions

    Synthesis and SAR studies of benzimidazole derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists: Focus to detune hERG inhibition

    P. K. Sasmal, S. Sasmal, C. Abbineni, B. Venkatesham, P. T. Rao, M. Roshaiah, I. Khanna, V. J. Sebastian, J. Suresh, M. P. Singh, R. Talwar, D. Shashikumar, K. H. Reddy, T. M. Frimurer, Ø. Rist, L. Elster and T. Högberg, Med. Chem. Commun., 2011, 2, 385
    DOI: 10.1039/C1MD00015B

Search articles by author

Spotlight

Advertisements