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

Medchemcomm. 2018 Dec 10;10(1):80-88. doi: 10.1039/c8md00328a. eCollection 2019 Jan 1.

Authors

Omobolanle J Jesumoroti¹, Faridoon¹, Dumisani Mnkandhla^{2

3}, Michelle Isaacs^{2

3}, Heinrich C Hoppe^{2

3}, Rosalyn Klein^{1

3}

Affiliations

¹ Department of Chemistry , Rhodes University , Grahamstown , 6140 , South Africa . Email: [email protected].
² Department of Biochemistry and Microbiology , Rhodes University , Grahamstown , 6140 , South Africa.
³ Centre for Chemico- and Biomedicinal Research , Rhodes University , Grahamstown , 6140 , 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.