2. Academic Validation
  3. Inhibition of HIV-1 RT activity by a new series of 3-(1,3,4-thiadiazol-2-yl)thiazolidin-4-one derivatives

Inhibition of HIV-1 RT activity by a new series of 3-(1,3,4-thiadiazol-2-yl)thiazolidin-4-one derivatives

  • Bioorg Med Chem. 2020 Apr 15;28(8):115431. doi: 10.1016/j.bmc.2020.115431.
Maria Rosa Buemi 1,  Rosaria Gitto 1,  Laura Ielo 2,  Christophe Pannecouque 3,  Laura De Luca 4
Affiliations

Affiliations

  • 1 Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Palatucci, 13, I-98168 Messina, Italy.
  • 2 Department of Pharmaceutical Chemistry, University of Vienna, Althanstrasse 14, A-1090 Vienna, Austria.
  • 3 Department of Microbiology and Immunology, Lab. of Virology and Chemotherapy, Rega Institute for Medical Research, B-3000 Leuven, Belgium.
  • 4 Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Palatucci, 13, I-98168 Messina, Italy. Electronic address: ldeluca@unime.it.
PMID: 32197813 DOI: 10.1016/j.bmc.2020.115431
Abstract

Non-nucleoside Reverse Transcriptase inhibitors (NNRTIs) represent potent anti-HIV agents targeting HIV-1 Reverse Transcriptase (RT), a crucial Enzyme for the viral life cycle. We have previously identified a series of NNRTIs bearing a 2,3-diaryl-1,3-thiazolidin-4-one core and some compounds proved to be effective in inhibiting HIV-1 replication at micromolar concentration. As a continuation in this research work we report the design, the synthesis and the structure-activity relationship studies of a further series of 3-(1,3,4-thiadiazol-2-yl)thiazolidin-4-one derivatives containing an arylthioacetamide group as pharmacophoric structural requirement for binding to the RT catalytic area. The new compounds proved to be effective to inhibit RT activity at micromolar concentrations. Finally, docking studies were carried out in order to rationalize the biological results of the new synthesized inhibitors.

Keywords

Assays; HIV-1; Non-nucleoside reverse transcriptase inhibitors; Synthesis.

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