期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 14, 期 1, 页码 77-79出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2003.10.031
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资金
- NIAID NIH HHS [AI 40575] Funding Source: Medline
- NIGMS NIH HHS [GM 56495] Funding Source: Medline
A new class of methionine aminopeptidase (MetAP) inhibitors, which contain an internal hydroxamate (N-acyl-N-alkylhydroxylamine) core as the metal-chelating group, has been designed, synthesized, and tested. The compounds exhibited reversible, competitive inhibition against Escherichia coli MetAP as well as human MetAP-l and MetAP-2. The most potent inhibitor had a K-i value of 2.5 muM and > 20-fold selectivity toward E. coli MAP. (C) 2003 Elsevier Ltd. All rights reserved.
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