- Synthesis and evaluation of isoxazole derivatives as lysophosphatidic acid (LPA) antagonists
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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.
- Yamamoto, Takashi,Fujita, Koichi,Asari, Sayaka,Chiba, Akira,Kataba, Yuka,Ohsumi, Koji,Ohmuta, Naoko,Iida, Yuko,Ijichi, Chiori,Iwayama, Satoshi,Fukuchi, Naoyuki,Shoji, Masataka
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p. 3736 - 3740
(2008/02/07)
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- Novel azole compound
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Azole compounds represented by formula I: wherein ring A is isoxazole and the like, R1 is a substituted or unsubstituted aryl group and the like, R2 is a hydrogen atom and the like, and R3 is a substituted or unsubstituted alkyl group and the like, and pharmaceutically acceptable salts thereof inhibit the physiological activity of lysophosphatidic acid (LPA), and are useful as for the prophylaxis or treatment of diseases in which inhibition of the physiological activity of LPA is useful for the prophylaxis or treatment thereof, such as diseases involving the LPA receptor.
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Page/Page column 34
(2008/06/13)
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