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A series of novel pyrazole‐based lipoprotein‐associated phospholipase A2 (Lp‐PLA2) inhibitors have been designed and synthetized by a variety of acetophenones via a 10‐step convergent approach. The synthetic approach is carefully optimized, and an unsuccessful alternative route is also discussed. The in vitro biological activity reveals that all the synthesized compounds are potent Lp‐PLA2 inhibitors...
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