期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 13, 页码 3531-3535出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.04.144
关键词
Nocathiacin; Water-soluble; Thiazolyl peptide; Antibacterial
Novel water-soluble amide analogs were synthesized from nocathiacin I (1) through the formation of the carboxylic acid intermediate followed by coupling to primary or secondary amines. Several compounds with potent antibacterial activity and adequate water solubility were identified. Of these, compound 19 was selected for more extensive evaluation because of its excellent in vitro antibacterial activity and in vivo efficacy, as well as clean off-target screening. (C) 2009 Elsevier Ltd. All rights reserved.
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