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Updated: Aug 21, 2026

Synthesis and Assay of Vibrio Quorum Sensing Inhibitors
Published on: May 31, 2024
Synthesis and biological evaluation of novel propylamine derivatives as orally active squalene synthase inhibitors
Tsukasa Ishihara1, Hirotoshi Kakuta, Hiroshi Moritani
1Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd, Chemistry Laboratories, 21 Miyukigaoka, Tsukuba, Ibaraki 305-8585, Japan. ishihat@yamanouchi.co.jp
Abstract:
Squalene synthase inhibitors are potentially superior hypolipidemic agents. We synthesized novel propylamine derivatives, as well as evaluated their ability to inhibit squalene synthase and their lipid-lowering effects in rats. 1-Allyl-2-[3-(benzylamino)propoxy]-9H-carbazole (YM-75440) demonstrated potent inhibition of the enzyme derived from HepG2 cells with an IC(50) value of 63 nM. It significantly reduced both plasma total cholesterol and plasma triglyceride levels following oral dosing to rats with a reduced tendency to elevate plasma transaminase levels.
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