[Synthesis and vasodilative activities of benzamide derivatives].
Twenty two benzamide derivatives were synthesized of which twenty one were not reported before. Vasodilative activity screening in vitro has shown that most of the compounds possess various activities, among which compound H1, H11, H17, E1, E3 demonstrated a superior pharmacological profile to the lead compound when inhibiting effect on the noradrenaline (10(-7) mol.L-1) induced contraction of rat aortic strip was chosen as the evaluation criterion, while H7,15, E7 exerted significant inhibiting action toward 85.7 mmol.L-1 KCl induced contraction of rat aortic strip. Further evaluation assays for their KCO potentials showed that E1 might be an ATP sensitive KCO. Preliminary structure-activity relationships of this kind of aromatic amides are discussed herein.
He
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Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050.
Lin
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Z
Zhu
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L
Fu
H
H
D000818:Animals; D001011:Aorta / Q000187:drug effects; D001549:Benzamides / Q000138:chemical synthesis* / Q000494:pharmacology; D066298:In Vitro Techniques; D009119:Muscle Contraction / Q000187:drug effects; D051381:Rats; D014665:Vasodilator Agents / Q000138:chemical synthesis* / Q000494:pharmacology
D001549:Benzamides; D014665:Vasodilator Agents