Bioorganic and Medicinal Chemistry Letters p. 1291 - 1295 (2007)
Update date:2022-07-30
Topics:
Lee, Sunkyung
Kim, Taemi
Lee, Byung Ho
Yoo, Sung-eun
Lee, Kyunghee
Yi, Kyu Yang
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.
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(1972)