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Synthesis and evaluation of isoxazole derivatives as lysophosphatidic acid (LPA) antagonists
Authors:Yamamoto Takashi  Fujita Koichi  Asari Sayaka  Chiba Akira  Kataba Yuka  Ohsumi Koji  Ohmuta Naoko  Iida Yuko  Ijichi Chiori  Iwayama Satoshi  Fukuchi Naoyuki  Shoji Masataka
Affiliation:Pharmaceutical Research Laboratories, Ajinomoto Company Inc., 1-1 Suzuki-cho, Kawasaki-ku, Kawasaki-shi 210-8681, Japan.
Abstract: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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