2-(Peptidamido)-cyclobutanones: A novel strategy for the inhibition of serine elastases

Autor:	Lorne S. Reid, Henry W. Pauls, Bill Cheng
Rok vydání:	1992
Předmět:	chemistry.chemical_classification biology Stereochemistry Organic Chemistry Elastase Biochemistry Ring strain Serine Inhibitory potency Enzyme chemistry Enzyme inhibitor Drug Discovery biology.protein Potency Molecular Biology
Zdroj:	Bioorganic Chemistry. 20:124-134
ISSN:	0045-2068
DOI:	10.1016/0045-2068(92)90033-y
Popis:	The synthesis of 2-peptidamidocyclobutanones is described as a novel class of competitive elastase inhibitors. Their inhibitory potency, although modest (i.e., micromolar range), is up to two orders of magnitude better than their acyclic analogues. The enhanced potency is explained, in part, by the tendency of an sp2 hybrdized cyclobutyl carbonyl to release internal ring strain by conversion to an sp3 hybridized center.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::1462f71943610d21e0579e0cac13901d https://doi.org/10.1016/0045-2068(92)90033-y Zobrazit plný text záznamu