Chemical and Pharmaceutical Bulletin p. 2475 - 2482 (1994)
Update date:2022-08-16
Topics:
Nakajima
Izawa
Kashiwabara
Nakajima
Munezuka
Various heteroaromatic cyanoamidines were synthesized starting from nitriles via cyanoimidates or from amides via thioamides. The compounds were tested for inhibitory effect on the 40 mM K+-induced contraction of rat aorta strips and selected compounds were also evaluated for antagonism of the norepinephrine-induced contraction. Most of the cyanoamidines showed vasodilatory activities. Potent vasoactive compounds were also examined for stimulation of the 86Rb+ efflux to determine their potassium channel opening actions. Maximum potency was displayed by N-cyano-N'-(2-nitroxyethyl)-3-pyridinecarboxamidine (3h). The methanesulfonate of 3h, which was designated as KRN2391, has been selected for further development as an antianginal agent.
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Doi:10.1039/C19680000258
()Doi:10.1016/S0040-4039(01)91785-X
(1974)Doi:10.1016/j.molcatb.2013.02.002
(2013)Doi:10.1039/c6ra07081g
(2016)Doi:10.1039/c2cc34765b
(2012)Doi:10.1021/ja01182a069
(1948)
