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  • Title: Discovery and SAR studies of methionine-proline anilides as dengue virus NS2B-NS3 protease inhibitors.
    Author: Zhou GC, Weng Z, Shao X, Liu F, Nie X, Liu J, Wang D, Wang C, Guo K.
    Journal: Bioorg Med Chem Lett; 2013 Dec 15; 23(24):6549-54. PubMed ID: 24268549.
    Abstract:
    A series of methionine-proline dipeptide derivatives and their analogues were designed, synthesized and assayed against the serotype 2 dengue virus NS2B-NS3 protease, and methionine-proline anilides 1 and 2 were found to be the most active DENV 2 NS2B-NS3 competitive inhibitors with Ki values of 4.9 and 10.5 μM. The structure and activity relationship and the molecular docking revealed that L-proline, L-methionine and p-nitroaniline in 1 and 2 are the important characters in blocking the active site of NS2B-NS3 protease. Our current results suggest that the title dipeptidic scaffold represents a promising structural core to discover a new class of active NS2B-NS3 competitive inhibitors.
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