Phenolic P2/P3 core motif as thrombin inhibitors--design, synthesis, and X-ray co-crystal structure |
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| Authors: | Hanessian Stephen Therrien Eric van Otterlo Willem A L Bayrakdarian Malken Nilsson Ingemar Fjellström Ola Xue Yafeng |
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| Affiliation: | Department of Chemistry, Université de Montréal, C.P. 6128, Succ. Centre-Ville, Montréal, PQ, Canada H3C 3J7. stephen.hanessian@umontreal.ca |
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| 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. |
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