2. Academic Validation
  3. Synthesis and evaluation of isoxazole derivatives as lysophosphatidic acid (LPA) antagonists

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

  • Bioorg Med Chem Lett. 2007 Jul 1;17(13):3736-40. doi: 10.1016/j.bmcl.2007.04.024.
Takashi Yamamoto 1,  Koichi Fujita,  Sayaka Asari,  Akira Chiba,  Yuka Kataba,  Koji Ohsumi,  Naoko Ohmuta,  Yuko Iida,  Chiori Ijichi,  Satoshi Iwayama,  Naoyuki Fukuchi,  Masataka Shoji
Affiliations

Affiliation

  • 1 Pharmaceutical Research Laboratories, Ajinomoto Company Inc., 1-1 Suzuki-cho, Kawasaki-ku, Kawasaki-shi 210-8681, Japan.
PMID: 17467986 DOI: 10.1016/j.bmcl.2007.04.024
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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