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 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.

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.Figure optionsDownload as PowerPoint slide