Design, synthesis, and biological evaluation of novel dual inhibitors of secretory phospholipase A2 and sphingomyelin synthase

Gao Xing; Gong Haojun; Men Peng; Zhou Lu; Ye Deyong

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Design, synthesis, and biological evaluation of novel dual inhibitors of secretory phospholipase A2 and sphingomyelin synthase

Gao Xing,Gong Haojun,Men Peng,Zhou Lu,Ye Deyong * #

School of Pharmacy, Fudan University, Shanghai, 201203

*Correspondence author

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Funding: National Natural Science Foundation of China （No.Grants No.30973641, 20902013), Specialized Research Fund for the Doctoral Program of Higher Education）

Opened online:19 February 2013

Accepted by: none

Citation: Gao Xing,Gong Haojun,Men Peng.Design, synthesis, and biological evaluation of novel dual inhibitors of secretory phospholipase A2 and sphingomyelin synthase[OL]. [19 February 2013] http://en.paper.edu.cn/en_releasepaper/content/4519052

The secretory phospholipase A2 (sPLA2) and sphingomyelin (SMS) are the key enzymes to atherosclerosis. A novel series of eight sPLA2 and SMS dual inhibitors containing indole and α-amino cyanide fragments respectively with different length carbon chain and substitution position were designed and synthesized. In vitro biological evaluation showed that all the compounds provided inhibitory effects against both SMS and sPLA2, in which, the SMS inhibitory activities were better than the positive control compound D609. The compounds 5b and 5e had moderate SMS inhibitory effects in liver homogenate and in SMS2 high expression cell homogenate respectively, as well as had ideal sPLA2 inhibitory activities.

Keywords:atherosclerosis; secretory phospholipase A2 (sPLA2); sphingomyelin synthase (SMS); multi-target drug design; dual inhibitors

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