Design and optimization of quinazoline derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists: Part 2

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• 作者：Sanjita Sasmal^a ; D. Balasubrahmanyam^a ; Hariprasada R. Kanna Reddy^a ; Gade Balaji^a ; Gujjary Srinivas^a ; Srisailam Cheera^a ; Chandrasekhar Abbineni^a ; Pradip K. Sasmal^a ; ^&dagger ; ; ^{pradipks@drreddys.com} ; ^{sasmalpk@yahoo.co.in} ; Ish Khanna^a ; V.J. Sebastian^a ; Vikram P. Jadhav^a ; Manvendra P. Singh^a ; Rashmi Talwar^a ; J. Suresh^a ; Dhanya Shashikumar^a ; K. Harinder Reddy^a ; V. Sihorkar^a ; Thomas M. Frimurer^b ; Ø ; ystein Rist^b ; Lisbeth Elster^b ; Thomas Hö ; gberg^b ; ^&Dagger ; ; ^{thomas.hogberg@leo-pharma.com}
• 关键词：Melanin concentrating hormone (MCH) ; Quinazolines ; MCHR1 antagonists ; hERG ; Obesity
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 May, 2012
• 卷：22
• 期：9
• 页码：3163-3167
• 文件大小：1048 K

摘要

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.