Synthesis and antiviral activity of monobactams inhibiting the human cytomegalovirus protease. |
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Authors: | W W Ogilvie C Yoakim F D? B Haché L Lagacé J Naud J A O'Meara R Déziel |
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Affiliation: | Boehringer Ingelheim (Canada) Ltd., Bio-Méga Research Division, Laval, Québec, Canada. wogilvie@bio-mega.boehringer-ingelheim.ca |
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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. |
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