Synthesis and SAR of 1, 3-thiazolyl thiophene and pyridine derivatives as potent, orally active and S1P 3-sparing S1P 1 agonists

…, R Inoue, H Yuita, K Oguchi-Oshima, R Kaneko…

文献索引：Asano, Masayoshi; Nakamura, Tsuyoshi; Sekiguchi, Yukiko; Mizuno, Yumiko; Yamaguchi, Takahiro; Tamaki, Kazuhiko; Shimozato, Takaichi; Doi-Komuro, Hiromi; Kagari, Takashi; Tomisato, Wataru; Inoue, Ryotaku; Yuita, Hiroshi; Oguchi-Oshima, Keiko; Kaneko, Reina; Nara, Futoshi; Kawase, Yumi; Masubuchi, Noriko; Nakayama, Shintaro; Koga, Tetsufumi; Namba, Eiko; Nasu, Hatsumi; Nishi, Takahide Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 9 p. 3083 - 3088

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被引用次数: 8

摘要

We have previously disclosed 1, 2, 4-oxadiazole derivative 3 as a potent S1P3-sparing S1P1 agonist. Although compound 3 exhibits potent and manageable immunosuppressive efficacy in various in vivo models, recent studies have revealed that its 1, 2, 4-oxadiazole ring is subjected to enterobacterial decomposition. As provisions for unpredictable issues, a series of alternative compounds were synthesized on the basis of compound 3. Extensive ...