Synthesis and in vitro antiviral evaluation of 4-substituted 3,4-dihydropyrimidinones |
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Authors: | Dhanabal Kumarasamy Biswajit Gopal Roy Joana Rocha-Pereira Johan Neyts Satheeshkumar Nanjappan Subhasis Maity Musfiqua Mookerjee Lieve Naesens |
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Affiliation: | 1. Department of Pharmaceutical Chemistry, NSHM College of Pharmaceutical Technology, 124, B.L Saha Road, Kolkata 700053, India;2. Department of Chemistry, School of Physical Sciences, Sikkim University, 6th Mile, Tadong, Gangtok, Sikkim 737102, India;3. Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, Leuven 3000, Belgium;4. Department of Pharmaceutical Analysis, National Institute of Pharmaceutical Education and Research [NIPER-H], Balanagar, Hyderabad 500037, India |
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Abstract: | A series of 4-substituted 3,4-dihydropyrimidine-2-ones (DHPM) was synthesized, characterized by IR, 1H NMR, 13C NMR and HRMS spectra. The compounds were evaluated in vitro for their antiviral activity against a broad range of DNA and RNA viruses, along with assessment for potential cytotoxicity in diverse mammalian cell lines. Compound 4m, which possesses a long lipophilic side chain, was found to be a potent and selective inhibitor of Punta Toro virus, a member of the Bunyaviridae. For Rift Valley fever virus, which is another Bunyavirus, the activity of 4m was negligible. DHPMs with a C-4 aryl moiety bearing halogen substitution (4b, 4c and 4d) were found to be cytotoxic in MT4 cells. |
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Keywords: | Dihydropyrimidinones DHPM Antiviral activity Cytotoxicity Bunyavirus URMNHHAUVFEMIG-UHFFFAOYSA-N BAKBIOFRSIUKMG-UHFFFAOYSA-N JYWSCUFVWRZFDR-UHFFFAOYSA-N COXDUHVXCKQHRJ-UHFFFAOYSA-N PRLATGWSLBXBHB-UHFFFAOYSA-N ZBBPICFYDJFWNE-UHFFFAOYSA-N OZRQMWIPQPVTRT-UHFFFAOYSA-N MFTFMXXRCSLQAZ-MDZDMXLPSA-N FOHKYBGQFPYEOE-UHFFFAOYSA-N DIDVRNLWJBGGQJ-UHFFFAOYSA-N JFHAMNVZHGKQDQ-UHFFFAOYSA-N DQLQOHIBDUGYGF-UHFFFAOYSA-N XGPRBKIBJHTTMT-UHFFFAOYSA-N PRBINTYBUYEJNZ-UHFFFAOYSA-N |
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