Design, Synthesis and Biological Evaluation of Novel Substituted N,N′-Diaryl ureas as Potent p38 Inhibitors

Molecules

Dianxi Zhu²  Xingzhou Li¹  Wu Zhong¹  Dongmei Zhao² 

[1] Laboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China; E-Mail:;Key Laboratory of Structure-Based Drug Design and Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China; E-Mail:

关键词: kinase inhibitor;    p38 inhibitors;    p38 MAPK;    TNF-α;    glycine flip;   

DOI  :  10.3390/molecules200916604

来源: mdpi

【 摘 要 】

A novel series of substituted N,N′-diaryl ureas that act as p38α inhibitors have been designed and synthesized based on two key residues (Gly110 and Thr106) that are different in p38α MAPK than in other kinases. Preliminary biological evaluation indicated that most compounds possessed good p38α inhibitory potencies. Among these compounds, 9g appeared to be the most powerful and is the main compound that we will study in the future.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.