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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Lee S,Kim T,Lee BH,Yoo SE,Lee K,Yi KY

doi

10.1016/j.bmcl.2006.12.012

subject

Has Abstract

pub_date

2007-03-01 00:00:00

pages

1291-5

issue

5

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(06)01391-6

journal_volume

17

pub_type

杂志文章

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