Synthesis and evaluation of isoxazole derivatives as lysophosphatidic acid (LPA) antagonists.

Takashi Yamamoto,Koichi Fujita, Sayaka Asari,Akira Chiba, Yuka Kataba, Koji Ohsumi,Naoko Ohmuta, Yuko Iida,Chiori Ijichi,Satoshi Iwayama,Naoyuki Fukuchi,Masataka Shoji

Bioorganic & Medicinal Chemistry Letters（2007）

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摘要

A series of isoxazole derivatives were synthesized and their antagonistic activities against LPA stimulation on both LPA(1)/CHO cells and rHSC cells were evaluated. Among them, 3-(4-[4-[1-(2-chloro-cyclopent-1-enyl)-ethoxycarbonylamino]-isoxazol-3- y]]-benzylsulfanyl)-propionic acid (34) showed the most potent activities.

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关键词

lysophosphatidic acid,lysophosphatidic acid receptor (LPA1),LPA antagonists,isoxazole derivative,liver fibrosis

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