2-(Aryl)-3-furan-2-ylmethyl-thiazolidin-4-ones as selective HIV-RT Inhibitors

A series of 4-thiazolidinones were evaluated as selective inhibitors of the HIV-RT enzyme. Our attempt in correlating the derived physicochemical properties with the HIV-RT inhibitory activity resulted in some statistically significant QSAR models with good predictive ability. The QSAR studies indicated the role of lipophilicity, dipole moment and out-of-plane potential energy of the compounds in rationalizing the activity. One of the compounds, 1, inhibited the enzyme at 0.204 μM concentration with minimal toxicity to MT-4 cells.

In the present study, 4-thiazolidinones have been assembled by DCC-mediated three-component reaction of amine, aldehyde and mercapto acetic acid and tested as HIV-RT inhibitors.Figure optionsDownload as PowerPoint slide