134168-99-3Relevant academic research and scientific papers
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.
Nickel(II)-Catalyzed Synthesis of Unsymmetrical Carbodiimides Using Molecular Oxygen as an Oxidant from Isocyanides and Primary Amines
Kiyoi, Takao,Seko, Norihiko,Yoshino, Kohichiro,Ito, Yoshihiko
, p. 5118 - 5120 (2007/10/02)
In the course of our studies of a practical synthesis of the antihypertensive drug 1, a general and convenient preparation of N,N'-disubstituted carbodiimides 2 was achieved by the nickel(II)-catalyzed reaction of isocyanides with primary amines, using ox
Novel cyanoguanidine derivatives
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, (2008/06/13)
Compounds of the formula: STR1 wherein R1 and R2 are independently fluorine, chlorine or bromine atom, and R3 is a C4 -C7 alkyl having at least a branch at the C1 position, exhibit K+ channel opening activity and are useful as hypotensive agents and coronary vasodilators.
