Synthesis and evaluation of isoxazole derivatives as lysophosphatidic acid (LPA) antagonists.
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.
Yamamoto
Takashi
T
Pharmaceutical Research Laboratories, Ajinomoto Company Inc., 1-1 Suzuki-cho, Kawasaki-ku, Kawasaki-shi 210-8681, Japan.
Fujita
Koichi
K
Asari
Sayaka
S
Chiba
Akira
A
Kataba
Yuka
Y
Ohsumi
Koji
K
Ohmuta
Naoko
N
Iida
Yuko
Y
Ijichi
Chiori
C
Iwayama
Satoshi
S
Fukuchi
Naoyuki
N
Shoji
Masataka
M
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
D007555:Isoxazoles; D008246:Lysophospholipids; D011422:Propionates; C029658:propionic acid; C032881:lysophosphatidic acid