| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1362952 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
A series of 9-dihydroerythromycin A and B analogues with modification of the desosamine nitrogen have been synthesized and screened for motilin agonist activity, antibiotic activity, tachyphylaxis and hERG channel current inhibition. Small alkyl groups resulted in the potency while compounds with a primary or secondary amine resulted in the low motilin agonist potency. Several compounds were identified as non-antibiotic motilin receptor agonists with minimal tachyphylaxis and low hERG interaction.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Yaoquan Liu, Yong Li, Yue Chen, Hao Zheng, Mark Claypool, David C. Myles, Christopher W. Carreras,