期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 5, 期 12, 页码 1334-1339出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml500422m
关键词
Spingosine-1-phosphate; S1P1 agonist; FTY720; fungolimod; Gilenya
S1P(1) is a validated target for treatment of autoimmune disease, and functional antagonists with superior safety and pharmacokinetic properties are being sought as second generation therapeutics. We describe the discovery and optimization of (7-benzyloxy-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acids as potent, centrally available, direct acting S1P(1) functional antagonists, with favorable pharmacokinetic and safety properties.
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