1026185-48-7Relevant articles and documents
Halogen-containing heteroaromatic carbenes of the 1,2,4-triazole series and their transformations
Glinyanaya, Nataliya V.,Korotkikh, Nikolai I.,Rayenko, Gennady F.,Rusanov, Eduard B.,Ryabitsky, Alexey B.,Shvaika, Oles P.
, p. 30841 - 30848 (2021/11/17)
A series of new stable halogenated carbenes, 1-tert-butyl-3,4-diaryl-1,2,4-triazol-5-ylidenes, has been synthesized. According to quantum chemical calculations, 4-(2,3,4-trifluorophenyl)-substituted 1-tert-butyl-3,4-diaryl-1,2,4-triazol-5-ylidene is the l
Synthesis and structure-activity relationships of novel phenylcyanoguanidine derivatives as potassium channel openers
Yoshiizumi, Kazuya,Ikeda, Shoji,Goto, Katsumi,Morita, Tominori,Nishimura, Noriyasu,Sukamoto, Takayuki,Yoshino, Kohichiro
, p. 2042 - 2050 (2007/10/03)
3,5-Di-substituted phenylcyanoguanidine derivatives with halogen, cyano, and/or nitro groups at the 3- and 5-positions of the benzene ring exhibited very strong smooth muscle relaxation activity in vitro, as compared to pinacidil. Among them, N-(3-chloro-5-cyanophenyl)-N'-cyano-N''-tert- pentylguanidine (5s) showed 27-fold more potent activity than pinacidil, and exhibited a stronger and more lasting antihypertensive effect than pinacidil by oral administration to spontaneously hypertensive rats. We propose a new pharmacophore model in which the essential factors for binding to the potassium channel are an NH and a bulky alkyl group.
