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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.

SUBMITTER: Kumarasamy D

PROVIDER: S-EPMC7127791 | biostudies-literature | 2017 Jan

REPOSITORIES: biostudies-literature

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

Kumarasamy Dhanabal D Roy Biswajit Gopal BG Rocha-Pereira Joana J Neyts Johan J Nanjappan Satheeshkumar S Maity Subhasis S Mookerjee Musfiqua M Naesens Lieve L

Bioorganic & medicinal chemistry letters 20161205 2

A series of 4-substituted 3,4-dihydropyrimidine-2-ones (DHPM) was synthesized, characterized by IR, <sup>1</sup>H NMR, <sup>13</sup>C 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 Buny ...[more]

PMID: 27979594

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