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

Omobolanle J. Jesumoroti; Faridoon; Dumisani Mnkandhla; Michelle Isaacs; Heinrich C. Hoppe; Rosalyn Klein

doi:10.1039/C8MD00328A

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

Omobolanle J. Jesumoroti,^a Faridoon,^a Dumisani Mnkandhla,^b^c Michelle Isaacs,^b^c Heinrich C. Hoppe^b^c and Rosalyn Klein*^a^c

Author affiliations

* Corresponding authors

^a Department of Chemistry, Rhodes University, Grahamstown, South Africa
E-mail: r.klein@ru.ac.za

^b Department of Biochemistry and Microbiology, Rhodes University, Grahamstown, South Africa

^c Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown, South Africa

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.

Supplementary files

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., 2019,10, 80-88

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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, 10, 80
DOI: 10.1039/C8MD00328A
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MedChemComm

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

Abstract

Supplementary files

Publication details

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

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