Design, synthesis and Na+/H+ exchanger isoform-1 inhibitory activity of feruloylagmatine analogues.
- Author:
Jia-Ming LI
1
;
Yong HE
;
Peng ZHOU
;
Yun-Gen XU
;
Jia-Zhi PENG
;
Ri-Zheng SHENG
Author Information
1. Anhui Key Laboratory of Traditional Chinese Medicine, Department of Pharmacy, Anhui University of Traditional Chinese Medicine, Hefei 230031, China. lijiaming2004@sina.com
- Publication Type:Journal Article
- MeSH:
Agmatine;
analogs & derivatives;
chemical synthesis;
chemistry;
pharmacology;
Animals;
Cardiotonic Agents;
chemical synthesis;
chemistry;
pharmacology;
Drug Design;
Female;
Male;
Molecular Structure;
Rats;
Rats, Sprague-Dawley;
Sodium-Hydrogen Exchangers;
antagonists & inhibitors;
Structure-Activity Relationship
- From:
Acta Pharmaceutica Sinica
2011;46(8):936-941
- 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.
