Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 5, Issue 12, Pages 1334-1339Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml500422m
Keywords
Spingosine-1-phosphate; S1P1 agonist; FTY720; fungolimod; Gilenya
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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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