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Identification of prostaglandin D2 receptor antagonists based on a tetrahydropyridoindole scaffold.

Abstract：

:A new series of indole-based antagonists of the PGD(2) receptor subtype 1 (DP1 receptor) was identified and the progress of the structure-activity relationship study to the identification of potent and selective antagonists is presented. Selective DP1 antagonists with high potency and selectivity were prepared. Of particular interest is the DP1 antagonist 26 with a K(i) value of 1 nM for the DP1 receptor and an IC(50) value of 4.6 nM in a DP1 functional assay for the inhibition of the PGD(2) induced cAMP production in platelet rich plasma (PRP).

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Beaulieu C,Guay D,Wang Z,Leblanc Y,Roy P,Dufresne C,Zamboni R,Berthelette C,Day S,Tsou N,Denis D,Greig G,Mathieu MC,O'Neill G

doi

10.1016/j.bmcl.2008.03.015

subject

Has Abstract

pub_date

2008-04-15 00:00:00

pages

2696-700

issue

8

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(08)00289-8

journal_volume

18

pub_type

杂志文章

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