Synthesis and antiviral activity of monobactams inhibiting the human cytomegalovirus protease.

Bioorg Med Chem

Boehringer Ingelheim (Canada) Ltd., Bio-Méga Research Division, Laval, Québec, Canada.

Published: August 1999

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.

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http://dx.doi.org/10.1016/s0968-0896(99)00094-2DOI Listing

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