Design and synthesis of monocyclic β-lactams as mechanism-based inhibitors of human cytomegalovirus protease
| Autor: | Alan D. Borthwick, Haloun Jin, Leonard Yuen, Tarek S. Mansour, Gordon G. Weingarten, Mirek Tomaszewski, Jean Bedard, Zhouhan Hu, Terry M. Haley, Wei Wang |
|---|---|
| Rok vydání: | 1998 |
| Předmět: |
Proteases
Stereochemistry Clinical Biochemistry Substituent Pharmaceutical Science beta-Lactams Biochemistry Chemical synthesis Substrate Specificity Serine Structure-Activity Relationship chemistry.chemical_compound Drug Stability Isomerism Drug Discovery Humans Structure–activity relationship Protease Inhibitors Molecular Biology chemistry.chemical_classification biology Serine Endopeptidases Organic Chemistry Enzyme chemistry Enzyme inhibitor biology.protein Lactam Molecular Medicine |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 8:365-370 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(98)00032-8 |
| Popis: | Mechanism based inhibitors of HCMV protease have been designed based on the monocyclic beta-lactam nucleus, which have been shown to acylate the viral enzyme in a time dependent manner. SAR in a series of monocyclic beta-lactam N-ureas, has defined the size and relative stereochemistry of the C-3 substituent producing a low micromolar inhibitor 17b with good aqueous stability and selectivity over the mammalian serine proteases. |
| Databáze: | OpenAIRE |
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