Potent and selective bicyclic lactam inhibitors of thrombin: Part 2: P1 modifications.

作者信息

Plummer J S, Berryman K A, Cai C, Cody W L, DiMaio J, Doherty A M, Edmunds J J, He J X, Holland D R, Levesque S, Kent D R, Narasimhan L S, Rubin J R, Rapundalo S T, Siddiqui M A, Susser A J, St-Denis Y, Winocour P D

机构信息

Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, MI 48105, USA.

出版信息

Bioorg Med Chem Lett. 1998 Dec 1;8(23):3409-14. doi: 10.1016/s0960-894x(98)00613-1.

DOI:10.1016/s0960-894x(98)00613-1

PMID:9873743

Abstract

The synthesis and antithrombotic activity of a series of nonpeptide bicyclic thrombin inhibitors is described. We have explored the SAR with modifications to the P1 site. The introduction of arginine mimetics at the P1 site led to potent and selective thrombin inhibitors.

摘要

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