1477811-41-8Relevant articles and documents
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
, p. 1164 - 1170 (2013/10/21)
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. The secretory phospholipase A2 (sPLA2) and sphingomyelin (SMS) are the key enzymes to atherosclerosis. In this paper, we combined the single sPLA2 and SMS inhibitors with a carbon chain to get a series of dual inhibitors. The biological evaluation showed these compounds had the moderate inhibition against both enzymes. Copyright
