文章基本信息

标题：Synthesis and potential biological activity of some novel 3-[(N-substituted indol-3-yl)methyleneamino]-6-amino4-aryl-pyrano(2,3-c)pyrazole-5-carbonitriles and 3,6-diamino4-(N-substituted indol-3-yl)pyrano(2,3-c)pyrazole-5-carbonitriles
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作者：ADEL HAMED MANDOUR ; ESLAM REDA EL-SAWY ; MANAL SHAABAN EBAID 等
期刊名称：Acta Pharmaceutica
电子版ISSN：1846-9558
出版年度：2012
卷号：62
期号：1
页码：15-30
DOI：10.2478/v10007-012-0007-0
语种：English
出版社：Sciendo
摘要：Starting from N-substituted indole-3-carboxaldehydes (1a-g) a series of new 3-[(N-substituted indol-3-yl)methyleneamino]-6-amino-4-aryl-pyrano(2,3-c)pyrazole-5-carbonitriles (3a-g and 4a-g) have been synthesized via the acid catalyzed condensation reaction of 1a-g with 3-amino-5-pyrazolone,followed by the reaction with arylidene malononitriles.A series of new 3,6-diamino-4-(N-substituted indol-3-yl)pyrano(2,3-c)pyrazole-5-carbonitriles (7a-g) have been prepared either via the base catalyzed condensation reaction of 1a-g with 3-amino-5-pyrazolone to give 6a-g,followed by the reaction with malononitrile or by the reaction of N-substituted-3-indolylidene malononitriles (5a-g) with 3-amino-5-pyrazolone.According to the obtained results,the newly synthesized compounds possess significant anti-inflammatory,analgesic and anticonvulsant activities.The anticonvulsant potency of certain tested compounds was more pronounced than both anti-inflammatory and analgesic activities.Moreover,most of the newly synthesized compounds possess potential antimicrobial activity against Escherichia coli and Pseudomonas aeruginosa.
关键词：indole;pyrano(2;3-c)pyrazole;anti-inflammatory;analgesic;anticonvulsant;antimicrobial activity