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Arylalkylidene rhodanine with bulky and hydrophobic functional group as selective HCVNS3 protease inhibitor

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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 11, 期 2, 页码 91-94

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(00)00610-7

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Arylalkylidene rhodanines 2(a-d) inhibit HCV NS3 protease at moderate concentrations. They are better inhibitors of other serine proteases such as chymotrypsin and plasmin. However, the selectivity of arylmethylidene rhodanines (8a, 9a) with bulkier and more hydrophobic functional groups increases by 13- and 25-fold towards HCV NS3 protease respectively. (C) 2001 Elsevier Science Ltd. All rights reserved.

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