Synthesis and in vitro antiviral evaluation of 4-substituted 3,4-dihydropyrimidinones

Bioorg Med Chem Lett. 2017 Jan 15;27(2):139-142. doi: 10.1016/j.bmcl.2016.12.010.

Dhanabal Kumarasamy ¹, Biswajit Gopal Roy ², Joana Rocha-Pereira ³, Johan Neyts ³, Satheeshkumar Nanjappan ⁴, Subhasis Maity ⁵, Musfiqua Mookerjee ⁵, Lieve Naesens ³

Affiliations

1 Department of Pharmaceutical Chemistry, NSHM College of Pharmaceutical Technology, 124, B.L Saha Road, Kolkata 700053, India. Electronic address: [email protected].
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.
5 Department of Pharmaceutical Chemistry, NSHM College of Pharmaceutical Technology, 124, B.L Saha Road, Kolkata 700053, India.

PMID: 27979594 DOI: 10.1016/j.bmcl.2016.12.010

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.

Keywords

Antiviral activity; Bunyavirus; Cytotoxicity; DHPM; Dihydropyrimidinones.

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