Add time:08/23/2019         Source:sciencedirect.com

A novel, potent and selective quinazolinone series of inhibitors of p38α MAP kinase has been identified. Modifications designed to address the issues of poor aqueous solubility and high plasma protein binding as well as embedded aniline functionalities resulted in the identification of a clinical candidate N-cyclopropyl-4-methyl-3-[6-(4-methylpiperazin-1-yl)-4-oxoquinazolin-3(4H)-yl]benzamide (AZD6703). Optimisation was guided by understanding of the binding modes from X-ray crystallographic studies which showed a switch from DFG ‘out’ to DFG ‘in’ as the inhibitor size was reduced to improve overall properties.

We also recommend Trading Suppliers and Manufacturers of Methyl 1-ethyl-6-fluoro-7-(4-Methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylate (cas 108224-80-2). Pls Click Website Link as below: cas 108224-80-2 suppliers