Positional Isomerism Confers Anti-HIV Activity of Some 4-hydroxycoumarin (4-hc) Derivatives in Cell Culture

摘要

Seventeen bis-(4-hydroxycoumarin) (4-hc) derivatives have been synthesized by interaction between 4-hc and aromatic aldehydes with different substituents in the aromatic nucleus. The condensation process was carried out in ethanol medium at reflux. The substances have been improved by the elemental analyses, IR-, 'H-NMR and mass spectral investigations. HIV integrase (IN) additionally to reverse transcriptase (RT) and protease (PR) came into the focus of researchers and a new class of inhibitors was identified - that of HIV-IN inhibitors. This prompted us to look for anti-HIV activity in cell culture of 17 4-hc. As a result, three 4-hc were found to exhibit anti-HIV activity, which was not linked to blocking of syncytium formation, or RT and PR inhibition. Studies are in progress to clarify activity to HIV-1 IN. Structurally, all three 4-hc were positional isomers of di- and three-methoxy-4-hc, probably conferring their anti-HIV activity.