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ID: ALA1148836

Journal: Bioorg Med Chem Lett

Title: 3-Substituted-(5-arylfuran-2-ylcarbonyl)guanidines as NHE-1 inhibitors.

Authors: Lee S, Kim T, Lee BH, Yoo SE, Lee K, Yi KY.

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 microM) that match those of 3-unsubstituted derivatives.

CiteXplore: 17189690

DOI: 10.1016/j.bmcl.2006.12.012