4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 16, Issue 4, Pages 1032-1036

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.10.082

Keywords

thrombin; inhibitor; trypsin; phenol; sulfonamide

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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. (c) 2005 Elsevier Ltd. All rights reserved.

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