Synthesis and antiviral activity of monobactams inhibiting the human cytomegalovirus protease

A series of monobactam inhibitors of HCMV (N-o) protease bearing a heterocy cle 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-b enzothiazole were found to be active in a plaque reduction assay. Furthermo re, 2-benzothiazole derivatives were shown to inhibit the HCMV protease act ivity inside cells by using a cell transfection assay, indicating that thei r antiviral activity in the plaque reduction assay could be attributed to p rotease inhibition. (C) 1999 Elsevier Science Ltd. All rights reserved.