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Synthesis and in vitro antiviral evaluation of 4-substituted 3,4-dihydropyrimidinones.
- 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.)
- Subjects :
- Animals
Antiviral Agents chemical synthesis
Antiviral Agents toxicity
Bunyaviridae drug effects
Cats
Chlorocebus aethiops
Dextran Sulfate pharmacology
Dogs
HeLa Cells
Humans
Mycophenolic Acid pharmacology
Pyrimidinones chemical synthesis
Pyrimidinones toxicity
Ribavirin pharmacology
Vero Cells
Antiviral Agents pharmacology
DNA Viruses drug effects
Pyrimidinones pharmacology
RNA Viruses drug effects
Subjects
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