Journal of Medicinal Chemistry p. 206 - 212 (1984)
Update date:2022-08-05
Topics:
Sablayrolles
Cros
Milhavet
Rechenq
Chapat
Boucard
Serrano
McNeill
A series of imidazo[1,2-a]pyrazine derivatives was synthesized by condensation of α-halogenocarbonyl compounds and aminopyrazines. Various compounds resulted from competitive reactions or reagent isomerization and demonstrated in vitro uterine-relaxing and in vivo antibronchospastic activities. On isolated atria, 5-bromoimidazo[1,2-a]pyrazine showed positive chronotropic and inotropic properties; the latter was associated with an increase in the cyclic AMP tissue concentration. Potentiation of the isoproterenol positive inotropic effect of 5-bromoimidazo[1,2-a]pyrazine and the lack of blockade of the 5-bromoimidazo[1,2-a]pyrazine positive inotropic effect by propranolol suggested phosphodiesterase-inhibiting properties.
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()Doi:10.1016/0022-328X(83)80242-3
(1983)