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(7-Benzyloxy-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic Acids as S1P1 Functional Antagonists.

ABSTRACT: S1P1 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 S1P1 functional antagonists, with favorable pharmacokinetic and safety properties.

SUBMITTER: Buzard DJ 

PROVIDER: S-EPMC4265824 | biostudies-other | 2014 Dec

REPOSITORIES: biostudies-other

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(7-Benzyloxy-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic Acids as S1P1 Functional Antagonists.

Buzard Daniel J DJ   Lopez Luis L   Moody Jeanne J   Kawasaki Andrew A   Schrader Thomas O TO   Kasem Michelle M   Johnson Ben B   Zhu Xiuwen X   Thoresen Lars L   Kim Sun Hee SH   Gharbaoui Tawfik T   Sengupta Dipanjan D   Calvano Lorene L   Krishnan Ashwin A   Gao Yinghong Y   Semple Graeme G   Edwards Jeff J   Barden Jeremy J   Morgan Michael M   Usmani Khawja K   Chen Chuan C   Sadeque Abu A   Chen Weichao W   Christopher Ronald J RJ   Thatte Jayant J   Fu Lixia L   Solomon Michelle M   Whelan Kevin K   Al-Shamma Hussien H   Gatlin Joel J   Gaidarov Ibragim I   Anthony Todd T   Le Minh M   Unett David J DJ   Stirn Scott S   Blackburn Anthony A   Behan Dominic P DP   Jones Robert M RM  

ACS medicinal chemistry letters 20141125 12

S1P1 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 S1P1 functional antagonists, with favorable pharmacokinetic and safety properties. ...[more]

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