| Literature DB >> 22497763 |
Sanjita Sasmal1, D Balasubrahmanyam, Hariprasada R Kanna Reddy, Gade Balaji, Gujjary Srinivas, Srisailam Cheera, Chandrasekhar Abbineni, Pradip K Sasmal, Ish Khanna, V J Sebastian, Vikram P Jadhav, Manvendra P Singh, Rashmi Talwar, J Suresh, Dhanya Shashikumar, K Harinder Reddy, V Sihorkar, Thomas M Frimurer, Øystein Rist, Lisbeth Elster, Thomas Högberg.
Abstract
Melanin concentrating hormone receptor 1 (MCHR1) antagonists have potential for the treatment of obesity and several CNS disorders. In the preceding article, we have described a novel series of quinazolines as MCHR1 antagonists and demonstrated in vivo proof of principle with an early lead. Herein we describe the detailed SAR and SPR studies to identify an optimized lead candidate having good efficacy in a sub-chronic DIO model with a good cardiovascular safety window.Entities:
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Year: 2012 PMID： 22497763 DOI： 10.1016/j.bmcl.2012.03.049
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823