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Article

Novel Thiazolidin-4-ones as Potential Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase

1
Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, Thessaloniki 54124, Greece
2
Department of Biomedical Sciences, School of Health Sciences, International Hellenic University, Nea Moudania 57001, Greece
3
Department of Pharmacology and Pharmacognosy, School of Pharmacy, Aristotle University of Thessaloniki, Thessaloniki 54124, Greece
*
Author to whom correspondence should be addressed.
Molecules 2019, 24(21), 3821; https://doi.org/10.3390/molecules24213821
Received: 30 August 2019 / Revised: 20 October 2019 / Accepted: 22 October 2019 / Published: 23 October 2019
Background: HIV is the causative agent of Acquired Immunodeficiency Syndrome (AIDS), an infectious disease with increasing incidence worldwide. Non-nucleoside reverse transcriptase inhibitors (NNRTIs) play an important role in the treatment of AIDS. Although, many compounds are already being used as anti-HIV drugs, research for the development of new inhibitors continues as the virus develops resistant strains. Methods: The best features of available NNRTIs were taken into account for the design of novel inhibitors. PASS (Prediction of activity spectra for substances) prediction program and molecular docking studies for the selection of designed compounds were used for the synthesis. Compounds were synthesized using conventional and microwave irradiation methods and HIV RT inhibitory action was evaluated by colorimetric photometric immunoassay. Results: The evaluation of HIV-1 RT inhibitory activity revealed that seven compounds have significantly lower ΙC50 values than nevirapine (0.3 μΜ). It was observed that the activity of compounds depends not only on the nature of substituent and it position in benzothiazole ring but also on the nature and position of substituents in benzene ring. Conclusion: Twenty four of the tested compounds exhibited inhibitory action lower than 4 μΜ. Seven of them showed better activity than nevirapine, while three of the compounds exhibited IC50 values lower than 5 nM. Two compounds 9 and 10 exhibited very good inhibitory activity with IC50 1 nM. View Full-Text
Keywords: thiazolidin-4-ones; NNRTIs; AIDS; HIV-1 reverse transcriptase; molecular docking thiazolidin-4-ones; NNRTIs; AIDS; HIV-1 reverse transcriptase; molecular docking
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MDPI and ACS Style

Petrou, A.; Eleftheriou, P.; Geronikaki, A.; Akrivou, M.G.; Vizirianakis, I. Novel Thiazolidin-4-ones as Potential Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase. Molecules 2019, 24, 3821. https://doi.org/10.3390/molecules24213821

AMA Style

Petrou A, Eleftheriou P, Geronikaki A, Akrivou MG, Vizirianakis I. Novel Thiazolidin-4-ones as Potential Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase. Molecules. 2019; 24(21):3821. https://doi.org/10.3390/molecules24213821

Chicago/Turabian Style

Petrou, Anthi, Phaedra Eleftheriou, Athina Geronikaki, Melpomeni G. Akrivou, and Ioannis Vizirianakis. 2019. "Novel Thiazolidin-4-ones as Potential Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase" Molecules 24, no. 21: 3821. https://doi.org/10.3390/molecules24213821

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