Letters in Drug Design & Discovery

Author(s): Eleni Pitta, Emmanuele Crespan, Athina Geronikaki, Giovanni Maga and Alberta Samuele

DOI: 10.2174/157018010790945869

Novel Thiazolidinone Derivatives with an Uncommon Mechanism of Inhibition Towards HIV-1 Reverse Transcriptase

Page: [228 - 234] Pages: 7

  • * (Excluding Mailing and Handling)

Abstract

Here, we show that novel 2-aryl-3-(4-adamantyl-thiazol-21,3-thiazolidin-4-one derivatives have a mixed- or fully competitive mechanism of inhibition towards HIV-1 Reverse Transcriptase with respect to the substrates of the reaction. Thus, they are interesting starting points for the development of novel NNRTIs with an uncommon mechanism of action.

Keywords: HIV-1 RT, HAART, NNRTIs, AIDS, Antiretroviral therapy, Enzyme kinetics