title: Synthesis and evaluation of isoxazole derivatives as lysophosphatidic acid (LPA) antagonists.
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.
authors.affiliation: Pharmaceutical Research Laboratories, Ajinomoto Company Inc., 1-1 Suzuki-cho, Kawasaki-ku, Kawasaki-shi 210-8681, Japan.
authors.forename: Takashi
authors.initials: T
authors.lastname: Yamamoto
authors.forename: Koichi
authors.initials: K
authors.lastname: Fujita
authors.forename: Sayaka
authors.initials: S
authors.lastname: Asari
authors.forename: Akira
authors.initials: A
authors.lastname: Chiba
authors.forename: Yuka
authors.initials: Y
authors.lastname: Kataba
authors.forename: Koji
authors.initials: K
authors.lastname: Ohsumi
authors.forename: Naoko
authors.initials: N
authors.lastname: Ohmuta
authors.forename: Yuko
authors.initials: Y
authors.lastname: Iida
authors.forename: Chiori
authors.initials: C
authors.lastname: Ijichi
authors.forename: Satoshi
authors.initials: S
authors.lastname: Iwayama
authors.forename: Naoyuki
authors.initials: N
authors.lastname: Fukuchi
authors.forename: Masataka
authors.initials: M
authors.lastname: Shoji
mesh_terms: D000818:Animals; D016466:CHO Cells; D049109:Cell Proliferation; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D006224:Cricetinae; D003412:Cricetulus; D015195:Drug Design; D005355:Fibrosis / Q000473:pathology; D006801:Humans; D020128:Inhibitory Concentration 50; D007555:Isoxazoles / Q000138:chemical synthesis* / Q000737:chemistry; D008099:Liver / Q000166:cytology; D008246:Lysophospholipids / Q000037:antagonists & inhibitors* / Q000737:chemistry; D011422:Propionates / Q000737:chemistry; D051381:Rats
chemical_list: D007555:Isoxazoles; D008246:Lysophospholipids; D011422:Propionates; C029658:propionic acid; C032881:lysophosphatidic acid