Design, Synthesis and Biological Actmty of Novel Rigid Amidino-Phenylalanine Derivatives as Inhibitors of Thrombin
- 1 January 1995
- journal article
- research article
- Published by Taylor & Francis in Journal of Enzyme Inhibition
- Vol. 9 (1), 73-86
- https://doi.org/10.3109/14756369509040682
Abstract
(3S)-(Naphthalene-2-sulfonylamino)-1-[2R-(4-amidinophenyl)-1-piperidinocarbonylethyl]-2-pyrroli-dinone (1a) is a potent inhibitor of thrombin with an IC50 value by 112 times lower than that of NAPAF’ (racemate). The selectivity versus trypsin can be improved by incorporation of substituents on the naphthyl ring. The mode of binding of the compound was determined by X-ray crystallography.Keywords
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