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Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists.

作者信息

Ahn H S, Arik L, Boykow G, Burnett D A, Caplen M A, Czarniecki M, Domalski M S, Foster C, Manna M, Stamford A W, Wu Y

机构信息

Schering-Plough Research Institute, Kenilworth, NJ 07033-0539, USA.

出版信息

Bioorg Med Chem Lett. 1999 Jul 19;9(14):2073-8. doi: 10.1016/s0960-894x(99)00339-x.

DOI:10.1016/s0960-894x(99)00339-x
PMID:10450984
Abstract

A series of pyrroloquinazolines has been discovered that represent novel small molecule inhibitors of the intramolecular ligand of the thrombin receptor. Analogs were prepared to study the structure-activity relationships of substitution at the N 1, N3, and N7 positions of the heterocycle. Compounds 4e and 4f have been identified with IC50's of 56 and 52 nM, respectively.

摘要

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