关键词: 喹啉, 乙酰胺P, 生物活性, 抑制剂, 磷酯酶

Phospholipase A2(PLA2) plays an important role in the pathology of a number of human diseases and is an attract target for medicinal chemistry research. Therefore, the development of novel tyep PLA2 inhibitors is of great interest for both bioorganic studies and clinical application. We focus on designing and synthesizing non- analogues of the phospholipidic substrate of sPLA2 n order to find new inhibitors. Herein, quinoline-4-acetamide sPLA2 inhibitors were designed by structure-based drug design method and synthesized. The structures of the title compounds were confirmed by elemental analysis, 1^H NMR, IR and MS. The preliminary bioassay data indicated that the title compounds display certain inhibition to sPLA2 at 10μ mol·L^-1 iv vitro, and were shown to active on animal model.

Key words: QUINOLINE, ACETAMIDE P, BIOLOGICAL ACTIVITY, INHIBITOR