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beta-Lactam derivatives as inhibitors of human cytomegalovirus protease
- Source :
- Journal of medicinal chemistry. 41(15)
- Publication Year :
- 1998
-
Abstract
- The development of novel monobactam inhibitors of HCMV protease incorporating a carbon side chain at C-4 and a urea function at N-1 is described. Substitution with small groups at the C-3 position of the beta-lactam ring gave an increase in enzymatic activity and in stability; however, a lack of selectivity against other serine proteases was noted. The use of both tri- and tetrasubstituted urea functionalities gave effective inhibitors of HCMV protease. Benzyl substitution of the urea moiety was beneficial, especially when strong electron-withdrawing groups where attached at the para position. Modest antiviral activity was found in a plaque reduction assay.
- Subjects :
- Proteases
Serine Proteinase Inhibitors
Stereochemistry
Swine
Cytomegalovirus
beta-Lactams
Antiviral Agents
Serine
chemistry.chemical_compound
Structure-Activity Relationship
Drug Discovery
medicine
Moiety
Monobactam
Animals
Humans
Urea
Cell Line, Transformed
chemistry.chemical_classification
biology
Chemistry
Serine Endopeptidases
Enzyme
Biochemistry
Enzyme inhibitor
Lactam
biology.protein
Molecular Medicine
Cattle
medicine.drug
Subjects
Details
- ISSN :
- 00222623
- Volume :
- 41
- Issue :
- 15
- Database :
- OpenAIRE
- Journal :
- Journal of medicinal chemistry
- Accession number :
- edsair.doi.dedup.....f03b5c600e50d12fe1a7e05cf5ae3d35