Abstract
Non-nucleoside reverse transcriptase inhibitors have a definitive role and most commonly used in treatment of HIV-1 infection. A new series of 4-ethylidene/substituted-benzylidene-1-(4-hydroxy/chloro-6-methylpyrimidin-2-yl)-2-ethyl/phenyl-1H-imidazol-5(4H)-one were designed, synthesized, and evaluated for HIV-1 reverse transcriptase (RT) inhibitory activity. The results of in-vitro HIV-1 RT assay showed that some of the new compounds, such as 4c, 4d, 4e, 5a, and 5e effectively inhibit HIV-1 RT activity. 1-(4-Chloro-6-methylpyrimidin-2-yl)-4-(furan-2-ylmethylene)-2-methyl-1H-imidazol-5(4H)-one (5e) exerted most potent in-vitro HIV-1 RT inhibitory activity, among the group of compounds. Molecular docking studies were carried out to explore the binding affinity of imidazole-5-one analogs in active site of HIV-1 RT enzyme.
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The authors are thankful to the Head, Department of Chemical Technology, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad 431004 (MS), India for providing the laboratory facility.
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Mokale, S.N., Lokwani, D.K. & Shinde, D.B. Synthesis, in-vitro reverse transcriptase inhibitory activity and docking study of some new imidazol-5-one analogs. Med Chem Res 23, 3752–3764 (2014). https://doi.org/10.1007/s00044-014-0954-8
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DOI: https://doi.org/10.1007/s00044-014-0954-8