Synthesis and SAR of 1,3-thiazolyl thiophene and pyridine derivatives as potent, orally active and S1P₃-sparing S1P₁ agonists.

Bioorganic & Medicinal Chemistry Letters(2012)

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摘要
A series of 1,3-thiazole derivatives were synthesized as potent, orally bioavailable S1P3-sparing S1P1 agonists. One of them, 24c, exhibited favorable efficacy in rat on host versus graft reaction (HvGR). The pharmacokinetic data for other compounds are shown as well.
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关键词
S1P1,Agonist,Lymphocyte,HvGR
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