title: [Design, synthesis and Na+/H+ exchanger isoform-1 inhibitory activity of feruloylagmatine analogues].
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.
authors: Anhui Key Laboratory of Traditional Chinese Medicine, Department of Pharmacy, Anhui University of Traditional Chinese Medicine, Hefei 230031, China. lijiaming2004@sina.com
authors: Jia-Ming
authors: JM
authors: Li
authors: Yong
authors: Y
authors: He
authors: Peng
authors: P
authors: Zhou
authors: Yun-Gen
authors: YG
authors: Xu
authors: Jia-Zhi
authors: JZ
authors: Peng
authors: Ri-Zheng
authors: RZ
authors: Sheng
mesh_terms: D000376:Agmatine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D002316:Cardiotonic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D005260:Female; D008297:Male; D015394:Molecular Structure; D051381:Rats; D017207:Rats, Sprague-Dawley; D017923:Sodium-Hydrogen Exchangers / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D002316:Cardiotonic Agents; D017923:Sodium-Hydrogen Exchangers; C419343:feruloylagmatine; C069139:growth factor-activatable Na-H exchanger NHE-1; D000376:Agmatine