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摘要:A novel series of eight SMS and sPLA2 dual inhibitors containing indole and a-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 fie ideal for liver homogenate and SMS2 high expression cell homogenate, respectively.
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