ChemInform Abstract: Metal Mediated Protease Inhibition: Design and Synthesis of Inhibitors of the Human Cytomegalovirus (hCMV) Protease

Autor:	Lisa T. Christmann, Kyle Elrod, Dashyant Dhanak, Richard M. Keenan, George Burton, Michael G. Darcy, Arun C. Kaura, Catherine E. Peishoff, Dinubhai H. Shah, John O. Link
Rok vydání:	2001
Předmět:	Proteases Protease Chymotrypsin biology Chemistry medicine.medical_treatment Elastase Biological activity General Medicine Trypsin In vitro Serine Biochemistry medicine biology.protein medicine.drug
Zdroj:	ChemInform. 32
ISSN:	1522-2667 0931-7597
Popis:	A versatile synthetic route to a novel series of bis-imidazolemethanes designed to inhibit the hCMV protease has been developed and a series of potential metal binding inhibitors has been identified. In selectivity assays, the compounds were highly specific for CMV protease and showed no inhibition (IC 50 >100 μM) of other prototypical serine proteases such as trypsin, elastase, and chymotrypsin. Although the presence of free zinc ions was found to be an absolute requirement for the in vitro biological activity of this class of inhibitor, the potency of the inhibitors could not be improved beyond the micromolar level.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::770795c81efaa1565aa1f3b8273e585b https://doi.org/10.1002/chin.200105104 Zobrazit plný text záznamu Plný text