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Evaluation of novel N′-(3-hydroxybenzoyl)-2-oxo-2H-chromene-3-carbohydrazide derivatives as potential HIV-1 integrase inhibitors

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Abstract

In an attempt to identify potential new agents that are active against HIV-1 IN, a series of novel coumarin-3-carbohydrazide derivatives were designed and synthesised. The toxicity profiles of these compounds showed that they were non-toxic to human cells and they exhibited promising anti-HIV-1 IN activities with IC50 values in nM range. Also, an accompanying molecular modeling study showed that the compounds bind to the active pocket of the enzyme.

Graphical abstract: Evaluation of novel N′-(3-hydroxybenzoyl)-2-oxo-2H-chromene-3-carbohydrazide derivatives as potential HIV-1 integrase inhibitors

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Publication details

The article was received on 03 Jul 2018, accepted on 01 Nov 2018 and first published on 10 Dec 2018


Article type: Research Article
DOI: 10.1039/C8MD00328A
Citation: Med. Chem. Commun., 2019, Advance Article
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    Evaluation of novel N′-(3-hydroxybenzoyl)-2-oxo-2H-chromene-3-carbohydrazide derivatives as potential HIV-1 integrase inhibitors

    O. J. Jesumoroti, Faridoon, D. Mnkandhla, M. Isaacs, H. C. Hoppe and R. Klein, Med. Chem. Commun., 2019, Advance Article , DOI: 10.1039/C8MD00328A

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