Significance of hydrogen bonding at the S-1 ' subsite of calpain I

Authors
Donkor, IO Zheng, XZ Han, J Lacy, C Miller, DD
Citation
Io. Donkor et al., Significance of hydrogen bonding at the S-1 ' subsite of calpain I, BIOORG MED, 11(13), 2001, pp. 1753-1755
Citations number
11
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
13
Year of publication
2001
Pages
1753 - 1755
Database
ISI
SICI code
0960-894X(20010709)11:13<1753:SOHBAT>2.0.ZU;2-H
Abstract
alpha -Ketohydroxamates were synthesized as bioisosteres of alpha -ketoamid es. The alpha -ketohydroxamates were generally more potent than the corresp onding alpha -ketoamides. The potency of the compounds suggests that hydrog en bonding and steric bulk of substituents on the nitrogen atom of the keto amide moiety influence calpain inhibition. (C) 2001 Elsevier Science Ltd. A ll rights reserved.