ChemInform Abstract: Synthesis and Structure-Activity Relationships of Thienylcyanoguanidine Derivatives as Potassium Channel Openers

Autor:	Noriyasu Nishimura, Kazuya Yoshiizumi, Kohichiro Yoshino, Shoji Ikeda
Rok vydání:	2010
Předmět:	Smooth muscle relaxation Stereochemistry organic chemicals Potassium chemistry.chemical_element General Medicine Thiophene derivatives Potassium channel In vitro chemistry.chemical_compound chemistry Pinacidil Thiophene heterocyclic compounds Benzene
Zdroj:	ChemInform. 29
ISSN:	1522-2667 0931-7597
DOI:	10.1002/chin.199823112
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::c1cb14626228e8cfbcde254b28cca3c6 https://doi.org/10.1002/chin.199823112 Zobrazit plný text záznamu Plný text