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 -hydroxy- and -ketoester functionalized thrombin inhibitors |
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| Authors: | Edwin J Iwanowicz James Lin Daniel G M Roberts Inge M Michel and Steven M Seiler |
| Institution: | Bristol-Myers Squibb Pharmaceutical Research Institute Princeton, NJ 08543-4000 USA |
| Abstract: | -Hydroxy- and -ketoester functionalized D-Phe-Pro-Lys tripeptides were found to be potent thrombin active site inhibitors. The ketoester derivatives were characterized by slow binding kinetics. The most potent of the series was 9 (BMS 181, 412) with an overall inhibition constant Ki* of 0.0017 μM. |
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