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  • Title: Design and synthesis of novel β-diketo derivatives as HIV-1 integrase inhibitors.
    Author: Hu L, Zhang S, He X, Luo Z, Wang X, Liu W, Qin X.
    Journal: Bioorg Med Chem; 2012 Jan 01; 20(1):177-82. PubMed ID: 22154762.
    Abstract:
    A series of novel β-diketo derivatives which combined the virtues of 1,3-diketo, 1,2,3-triazole and polyhydroxylated aromatics moieties, were designed and synthesized as potential HIV-1 integrase (IN) inhibitors and evaluated their inhibition to the strand transfer process of HIV-1 integrase. The result indicates that 3,4,5-trihydroxylated aromatic derivatives exhibit good inhibition to HIV-1 integrase, but dihydroxylated aromatic derivatives and corresponding methoxy aromatic derivatives appear little inhibition to HIV-1 integrase.
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