Synthesis and structure-activity relationships of thienylcyanoguanidine derivatives as potassium channel openers

Chemical & Pharmaceutical Bulletin
K YoshiizumiK Yoshino

Abstract

In our series of studies on potassium channel openers, several thienylcyanoguanidine derivatives were synthesized and evaluated for smooth muscle relaxation activity in vitro. Among the newly synthesized compounds, N-cyano-N'-(5-cyano-3-thienyl)-N"-tert-pentylguanidine (4b) and N-(5-bromo-3-thienyl)-N'-cyano-N"-tert-pentylguanidine (4f) exhibited excellent activity which was proved to be based on potassium channel-opening action. Bioisosterism between benzene and thiophene ring was observed in the arylcyanoguanidines. After intravenous administration to dogs, 4b lowered the blood pressure more strongly than pinacidil.

Citations

Nov 24, 2007·European Journal of Pharmacology·Florian WegnerAlexander Hoepping
May 28, 2004·Journal of Medicinal Chemistry·Tina M TagmoseJohn Bondo Hansen

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