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

Authors :
Kumarasamy D
Roy BG
Rocha-Pereira J
Neyts J
Nanjappan S
Maity S
Mookerjee M
Naesens L
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2017 Jan 15; Vol. 27 (2), pp. 139-142. Date of Electronic Publication: 2016 Dec 05.
Publication Year :
2017

Abstract

A series of 4-substituted 3,4-dihydropyrimidine-2-ones (DHPM) was synthesized, characterized by IR, <superscript>1</superscript> H NMR, <superscript>13</superscript> 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 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.<br /> (Copyright © 2016 Elsevier Ltd. All rights reserved.)

Details

Language :
English
ISSN :
1464-3405
Volume :
27
Issue :
2
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
27979594
Full Text :
https://doi.org/10.1016/j.bmcl.2016.12.010