Design and optimization of quinazoline derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists: Part 2
作者： Sanjita Sasmal , D. Balasubrahmanyam , Hariprasada R. Kanna Reddy , Gade Balaji , Gujjary Srinivas
DOI: 10.1016/J.BMCL.2012.03.049
关键词:
摘要: Melanin concentrating hormone (MCH) is an important mediator of energy homeostasis and plays a role in metabolic CNS disorders. The modeling-supported design, synthesis multi-parameter optimization (biological activity, solubility, stability, hERG) novel quinazoline derivatives as MCHR1 antagonists are described. vivo proof principle for weight loss with lead compound from this series exemplified. Clusters refined hMCHR1 homology models derived the X-ray structure β2-adrenergic receptor, including extracellular loops, were developed used to guide design.
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