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Design, Synthesis, and Biological Evaluation of Novel Dual Inhibitors of Secretory Phospholipase A2 and Sphingomyelin Synthase
Author(s) -
Gao Xing,
Gong Haojun,
Men Peng,
Zhou Lu,
Ye Deyong
Publication year - 2013
Publication title -
chinese journal of chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.28
H-Index - 41
eISSN - 1614-7065
pISSN - 1001-604X
DOI - 10.1002/cjoc.201300079
Subject(s) - chemistry , biochemistry , sphingomyelin , indole test , biological activity , in vitro , enzyme , stereochemistry , membrane
A novel series of eight SMS and sPLA2 dual inhibitors containing indole and α ‐amino cyanide fragments of different length and substitution position was synthesized and evaluated by three different in vitro assays. Biological evaluation showed that all compounds provided inhibitory effects against SMS (about 50% inhibition at 100 µmol/L) and sPLA2 (14–32 µmol/L). All the compounds had the SMS activity better than the positive control compound D609 in SMS2 homogenate, with compounds 5b and 5e ideal for liver homogenate and SMS2 high expression cell homogenate, respectively.