1374568-46-3

Upstream product

• 34790-24-4 4-methylquinazolin-2-ol 
• 551-93-9 2-aminoacetophenone 
• 69559-56-4 N-(2-acetylphenyl)-2,2,2-trichloroacetamide 
• 850172-43-9 4-methyl-6-nitroquinazolin-2-ol 
• 850172-44-0 2-chloro-4-methyl-6-nitroquinazoline 
• 40807-61-2 4-hydroxy-4-phenylpiperidin 

Downstream Products

• 1374568-14-5 C₂₀H₂₂N₄O 
• 1374855-88-5 (E)-3-(4-chlorophenyl)-N-(2-(4-hydroxy-4-phenylpiperidin-1-yl)-4-methylquinazolin-6-yl)acrylamide 

Relevant academic research and scientific papers

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

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.

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

Melanin concentrating hormone (MCH) is an important mediator of energy homeostasis and plays a role in metabolic and CNS disorders. The modeling-supported design, synthesis and multi-parameter optimization (biological activity, solubility, metabolic stability, hERG) of novel quinazoline derivatives as MCHR1 antagonists are described. The in vivo proof of principle for weight loss with a lead compound from this series is exemplified. Clusters of refined hMCHR1 homology models derived from the X-ray structure of the β2-adrenergic receptor, including extracellular loops, were developed and used to guide the design.