| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1372232 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
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.
Graphical abstractSynthesis and SAR of novel water-soluble amide analogs of nocathiacin 1 are reported. Compound 19 was selected for further evaluation.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Libo Xu, Amy K. Farthing, James F. Dropinski, Peter T. Meinke, Christine McCallum, Penny S. Leavitt, Emily J. Hickey, Lawrence Colwell, John Barrett, Kun Liu,