Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1378005 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
Abstract
The C-3 substituents effect on NHE-1 inhibitory activity of (5-arylfuran-2-ylcarbonyl)guanidines, previously identified as potent NHE-1 inhibitors, was investigated. The introduction of amine or alkyl groups at the 3-position of the furan ring, next to the acylguanidine moiety, remarkably improves NHE-1 inhibitory potency. Especially the important finding is that 5-(2,5-dichloro)phenyl and 5-(2-methoxy-5-chloro)phenyl derivatives exhibit high NHE-1 inhibitory activities (IC50 < 0.02 μM) that match those of 3-unsubstituted derivatives.
Graphical abstractThe synthesis and evaluation as NHE-1 inhibitors of 3-substituted-(5-arylfuran-2-ylcarbonyl)guanidines is described.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Sunkyung Lee, Taemi Kim, Byung Ho Lee, Sung-eun Yoo, Kyunghee Lee, Kyu Yang Yi,