Identification of benzoxazole analogs as novel, S1P(3) sparing S1P(1) agonists.

作者: Guanghui Deng , Qinghua Meng , Qian Liu , Xuesong Xu , Qiongfeng Xu

DOI: 10.1016/J.BMCL.2012.04.095

关键词:

摘要: A novel series of benzoxazole-derived S1P(1) agonists were designed based on scaffold hopping molecular design strategy combined with computational approaches. Extensive SAR studies led to the discovery compound 17d as a selective agonist (over S1P(3)) high CNS penetration and favorable DMPK properties. also demonstrated in vivo pharmacological efficacy reduce blood lymphocyte mice after oral administration.

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