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. 2014 Dec:57:1-4.
doi: 10.1016/j.bioorg.2014.07.008. Epub 2014 Jul 30.

Novel furocoumarins as potential HIV-1 integrase inhibitors

Temitope O Olomola  1 , Salerwe Mosebi  2 , Rosalyn Klein  1 , Telisha Traut-Johnstone  2 , Judy Coates  2 , Raymond Hewer  2 , Perry T Kaye  3
Affiliations

Novel furocoumarins as potential HIV-1 integrase inhibitors

Temitope O Olomola et al. Bioorg Chem. 2014 Dec.

Abstract

A series of seven novel, rationally designed N-substituted 3-{3,5-dimethylfuro[3,2-g]coumarin-6-yl}propanamides have been prepared as potential HIV-1 integrase (IN) inhibitors via a five-step pathway commencing with resorcinol and diethyl 2-acetylglutarate, and the HIV-1 IN inhibition potential of these compounds has been examined relative to raltegravir, a known HIV-1 IN inhibitor.

Keywords: Furocoumarins; HIV-1 integrase; Rational design; Strand-transfer inhibitors.

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