Design, synthesis and Na+/H+ exchanger isoform-1 inhibitory activity of feruloylagmatine analogues.
- Author:
Jiaming LI
;
Yong HE
;
Peng ZHOU
;
Yungen XU
;
Jiazhi PENG
;
Rizheng SHENG
- Publication Type:Journal Article
- From:
Acta Pharmaceutica Sinica
2011;46(8):936-41
- CountryChina
- Language:Chinese
-
Abstract:
In order to search for novel inhibitors of Na+/H+ exchanger isoform-1 (NHE-1), nine feruloylagmatine analogues were designed and synthesized from ferulic acid and agmatine. The structures of the synthesized compounds were confirmed by 1H NMR, 13C NMR and mass spectra, among which compounds 5f-5i were novel compounds. The results of preliminary pharmacological test showed that some of the compounds possessed strong NHE-1 inhibitory activity, among which compounds 5a, 5b and 6c were more potent than cariporide in NHE-1 inhibition.
