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

…, A Chiba, Y Kataba, K Ohsumi, N Ohmuta, Y Iida…

Index: Yamamoto, Takashi; Fujita, Koichi; Asari, Sayaka; Chiba, Akira; Kataba, Yuka; Ohsumi, Koji; Ohmuta, Naoko; Iida, Yuko; Ijichi, Chiori; Iwayama, Satoshi; Fukuchi, Naoyuki; Shoji, Masataka Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 13 p. 3736 - 3740

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Citation Number: 30

Abstract

A series of isoxazole derivatives were synthesized and their antagonistic activities against LPA stimulation on both LPA1/CHO cells and rHSC cells were evaluated. Among them, 3-(4- {4-[1-(2-chloro-cyclopent-1-enyl)-ethoxycarbonylamino]-isoxazol-3-yl}-benzylsulfanyl)- propionic acid (34) showed the most potent activities.