Phenolic P2/P3 core motif as thrombin inhibitors--design, synthesis, and X-ray co-crystal structure.

作者信息

Hanessian Stephen, Therrien Eric, van Otterlo Willem A L, Bayrakdarian Malken, Nilsson Ingemar, Fjellström Ola, Xue Yafeng

机构信息

Department of Chemistry, Université de Montréal, C.P. 6128, Succ. Centre-Ville, Montréal, PQ, Canada H3C 3J7.

出版信息

Bioorg Med Chem Lett. 2006 Feb 15;16(4):1032-6. doi: 10.1016/j.bmcl.2005.10.082. Epub 2005 Nov 15.

DOI:10.1016/j.bmcl.2005.10.082

PMID:16290930

Abstract

Prototypical thrombin inhibitors were synthesized based on a trisubstituted phenol as a core motif. A naphthylsulfonamide analogue showed excellent antithrombin activity. An X-ray co-crystal structure showed the expected interactions.

摘要

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