EXAMINATION OF PEPTIDIC ALPHA',BETA-DIAMINO-ALPHA,ALPHA-DIFLUOROKETONES AS INHIBITORS OF HUMAN-LEUKOCYTE ELASTASE

Authors
BERNSTEIN PR KOSMIDER BJ VACEK EP VEALE CA GOMES BC
Citation
Pr. Bernstein et al., EXAMINATION OF PEPTIDIC ALPHA',BETA-DIAMINO-ALPHA,ALPHA-DIFLUOROKETONES AS INHIBITORS OF HUMAN-LEUKOCYTE ELASTASE, Bioorganic & medicinal chemistry letters, 4(18), 1994, pp. 2175-2178
Citations number
14
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
18
Year of publication
1994
Pages
2175 - 2178
Database
ISI
SICI code
0960-894X(1994)4:18<2175:EOPA>2.0.ZU;2-O
Abstract
The preparation and in vitro evaluation of a series of peptidic alpha' ,beta-diamino-alpha,alpha-difluoroketones are described. Comparison of the efficacy of these compounds to both their corresponding trifluoro methylketone and alpha-carboxamido-alpha,alpha-difluoroketone inhibito rs reveals a divergent set of structure-activity relationships. This d ivergence indicates that the inhibitor's P-l'-amino group is strongly interacting with the enzyme's S-l'-subsite.