Abstract
A series of monobactam inhibitors of HCMV (N(o)) protease bearing a heterocycle linked by a methylene group at C-4 is described. Inhibitors containing a heterocycle such as a 2-furyl, 2-thiophenyl, 4-methyl-2-tetrazole and 2-benzothiazole were found to be active in a plaque reduction assay. Furthermore, 2-benzothiazole derivatives were shown to inhibit the HCMV protease activity inside cells by using a cell transfection assay, indicating that their antiviral activity in the plaque reduction assay could be attributed to protease inhibition.
MeSH terms
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Animals
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Antiviral Agents / chemical synthesis*
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Antiviral Agents / chemistry
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Antiviral Agents / pharmacology*
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COS Cells
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Cytomegalovirus / drug effects*
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Cytomegalovirus / enzymology
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Cytomegalovirus / growth & development
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Monobactams / chemical synthesis
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Monobactams / chemistry
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Monobactams / pharmacology
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Protease Inhibitors / chemical synthesis*
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Protease Inhibitors / chemistry
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Protease Inhibitors / pharmacology*
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Serine Endopeptidases / drug effects*
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Spectrum Analysis
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Viral Plaque Assay
Substances
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Antiviral Agents
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Monobactams
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Protease Inhibitors
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Serine Endopeptidases
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assemblin