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ID: ALA1131676

Journal: Bioorg Med Chem Lett

Title: The discovery of orally available thrombin inhibitors: optimisation of the P1 pharmacophore.

Authors: Ambler J, Bentley D, Brown L, Dunnet K, Farr D, Janus D, Le Grand D, Menear K, Mercer M, Talbot M, Tweed M, Wathey B.

Abstract: Thrombin inhibitors have been designed with the replacement of the strongly basic guanidine P1 pharmocophore with a group that exploits the lipophilicity of the S1 pocket. The approach has lead to the discovery of potent thrombin inhibitors demonstrating good intra-duodenal absorption.

CiteXplore: 10328293

DOI: 10.1016/s0960-894x(99)00138-9