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Himbacine derived thrombin receptor (PAR-1) antagonists: structure-activity relationship of the lactone ring.

Abstract：

:The structure-activity relationship (SAR) of the lactone ring of himbacine derived thrombin receptor (PAR-1) antagonists (e.g., 2-5) is described. The effect of the lactone carbonyl group on binding to PAR-1 is dependent on the substitution pattern of the pyridine ring. A stereoselective intramolecular Michael addition reaction to the vinyl pyridine group was observed for these pyridine analogs of himbacine in basic conditions at elevated temperature.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Xia Y,Chackalamannil S,Chan TM,Czarniecki M,Doller D,Eagen K,Greenlee WJ,Tsai H,Wang Y,Ahn HS,Boykow GC,McPhail AT

doi

10.1016/j.bmcl.2006.06.042

subject

Has Abstract

pub_date

2006-09-15 00:00:00

pages

4969-72

issue

18

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(06)00709-8

journal_volume

16

pub_type

杂志文章

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