Design and Synthesis of Novel Pyrazole-based Lp-PLA2 Inhibitors

✍ Scribed by Yi Wang; Weiren Xu; Hua Shao; Yafei Xie; Jianwu Wang

• Publisher: John Wiley and Sons
• Year: 2011
• Tongue: English
• Weight: 130 KB
• Volume: 29
• Category: Article
• ISSN: 0256-7660
• DOI: 10.1002/cjoc.201180354

✦ Synopsis

A series of novel pyrazole-based lipoprotein-associated phospholipase A 2 (Lp-PLA 2 ) inhibitors have been designed and synthetized by a variety of acetophenones via a 10-step convergent approach. The synthetic approach is carefully optimized, and an unsuccessful alternative route is also discussed. The in vitro biological activity reveals that all the synthesized compounds are potent Lp-PLA 2 inhibitors with compound 13b being the most potent one (Lp-PLA 2 , IC 50 ＝1.5 nmol/L).