63744-21-8Relevant articles and documents
Synthesis and Antibronchospastic Activity of 8-Alkoxy- and 8-(Alkylamino)imidazopyrazines
Bonnet, Pierre A.,Michel, Alain,Laurent, Florence,Sablayrolles, Claire,Rechencq, Eliane,et al.
, p. 3353 - 3358 (2007/10/02)
Theophylline still occupies a dominant place in asthma therapy.Unfortunatly its adverse central nervous system (CNS) stimulant effects can dramatically limit its use, and adjustments in the dosage are often needed.We have synthesized a new series of imidazopyrazine derivatives which are much more potent bronchodilators than theophylline in vivo and do not exhibit the CNS stimulatory profile.In vitro studies on isolated rat uterus and guinea pig trachea confirm the high potentialities of these derivatives. 6-Bromo-8-(methylamino)imidazopyrazine-3-carbonitrile (23) is identified as the most potent compound of the series.As i n the case of theophylline, phosphodiesterase inhibition appears unlikely to be the unique mechanism of the action of this series of heterocycles.
Synthesis of imidazo[1,2-a]pyrazine derivatives with uterine-relaxing, antibronchospastic, and cardiac-stimulating properties
Sablayrolles,Cros,Milhavet,Rechenq,Chapat,Boucard,Serrano,McNeill
, p. 206 - 212 (2007/10/02)
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.