FUROXANS AS NITRIC-OXIDE DONORS - 4-PHENYL-3-FUROXANCARBONITRILE - THIOL-MEDIATED NITRIC-OXIDE RELEASE AND BIOLOGICAL EVALUATION

被引:131
作者
MEDANA, C
ERMONDI, G
FRUTTERO, R
DISTILO, A
FERRETTI, C
GASCO, A
机构
[1] UNIV TURIN,DIPARTIMENTO SCI & TECNOL FARMACO,I-10125 TURIN,ITALY
[2] IST FARMACOL & TERAPIA SPERIMENTALE,I-10126 TURIN,ITALY
关键词
D O I
10.1021/jm00051a020
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
4-Phenyl-3-furoxancarbonitrile (2) affords nitric oxide under the action of thiol cofactors. Two principal products were isolated in the reaction with thiophenol: the phenylcyanoglyoxime (6) and 5-amino-3-phenyl-4-(phenylthio)isoxazol (7). Mechanisms which could account for the formation of these two products are discussed. Compound 2 is an efficient activator of the rat lung soluble guanylate cyclase, displays high vasodilatory activity on strips of rat thoracic aorta precontracted with noradrenaline, and is a potent inhibitor of platelet aggregation.
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页码:4412 / 4416
页数:5
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