Synthesis and biological evaluation of novel hybrid chalcone derivatives as vasorelaxant agents.
With the aim to further improve the vasorelaxant activities of chalcones, nine hybrid chalcone derivatives conjugated with nitric oxide (NO) donor or 1,4-dihydropyridyl (1,4-DHP) moiety were designed and synthesized based on molecular hybridization strategy. Their vasorelaxant activities were evaluated in aortic rings with endothelium pre-contracted with phenylephrine (PE). All of these compounds showed preferable vasorelaxant activities which were more potent than their parent compounds. Compounds 8c and 15c, the most potent compounds, would be promising structural templates for the development of novel vasorelaxant agents.
Dong
Xiaowu
X
ZJU-ENS Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
Du
Lilin
L
Pan
Zhichao
Z
Liu
Tao
T
Yang
Bo
B
Hu
Yongzhou
Y
D000818:Animals; D001011:Aorta / Q000187:drug effects / Q000502:physiology; D002599:Chalcone / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004095:Dihydropyridines / Q000737:chemistry; D008297:Male; D009569:Nitric Oxide / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship; D014665:Vasodilator Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D004095:Dihydropyridines; D014665:Vasodilator Agents; D009569:Nitric Oxide; D002599:Chalcone; C038806:1,4-dihydropyridine