Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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

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

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

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Article Details

VOLUME: 7
ISSUE: 4
Year: 2010
Page: [228 - 234]
Pages: 7
DOI: 10.2174/157018010790945869
Price: $58