title: Synthesis and in vitro antiviral evaluation of 4-substituted 3,4-dihydropyrimidinones.
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.
authors.affiliation: Department of Pharmaceutical Chemistry, NSHM College of Pharmaceutical Technology, 124, B.L Saha Road, Kolkata 700053, India. Electronic address: dhanabalrx@gmail.com.
authors.forename: Dhanabal
authors.initials: D
authors.lastname: Kumarasamy
authors.affiliation: Department of Chemistry, School of Physical Sciences, Sikkim University, 6th Mile, Tadong, Gangtok, Sikkim 737102, India.
authors.forename: Biswajit Gopal
authors.initials: BG
authors.lastname: Roy
authors.affiliation: Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, Leuven 3000, Belgium.
authors.forename: Joana
authors.initials: J
authors.lastname: Rocha-Pereira
authors.affiliation: Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, Leuven 3000, Belgium.
authors.forename: Johan
authors.initials: J
authors.lastname: Neyts
authors.affiliation: Department of Pharmaceutical Analysis, National Institute of Pharmaceutical Education and Research [NIPER-H], Balanagar, Hyderabad 500037, India.
authors.forename: Satheeshkumar
authors.initials: S
authors.lastname: Nanjappan
authors.affiliation: Department of Pharmaceutical Chemistry, NSHM College of Pharmaceutical Technology, 124, B.L Saha Road, Kolkata 700053, India.
authors.forename: Subhasis
authors.initials: S
authors.lastname: Maity
authors.affiliation: Department of Pharmaceutical Chemistry, NSHM College of Pharmaceutical Technology, 124, B.L Saha Road, Kolkata 700053, India.
authors.forename: Musfiqua
authors.initials: M
authors.lastname: Mookerjee
authors.affiliation: Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, Leuven 3000, Belgium.
authors.forename: Lieve
authors.initials: L
authors.lastname: Naesens
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D002043:Bunyaviridae / Q000187:drug effects; D002415:Cats; D002522:Chlorocebus aethiops; D004267:DNA Viruses / Q000187:drug effects*; D016264:Dextran Sulfate / Q000494:pharmacology; D004285:Dogs; D006367:HeLa Cells; D006801:Humans; D009173:Mycophenolic Acid / Q000494:pharmacology; D011744:Pyrimidinones / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D012328:RNA Viruses / Q000187:drug effects*; D012254:Ribavirin / Q000494:pharmacology; D014709:Vero Cells
chemical_list: D000998:Antiviral Agents; D011744:Pyrimidinones; C000622941:ethyl 6-methyl-2-oxo-4-undecyl-1,2,3,4-tetrahydro-5-pyrimidinecarboxylate; D012254:Ribavirin; D016264:Dextran Sulfate; D009173:Mycophenolic Acid
keywords: Antiviral activity; Bunyavirus; Cytotoxicity; DHPM; Dihydropyrimidinones