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一系列新型2-氨基-5-氧代-4-苯基-5,6,7,8-四氢喹啉-3-腈及其类似物的合成与抗真菌性能评价

Synthesis and evaluation of antifungal properties of a series of the novel 2-amino-5-oxo-4-phenyl-5,6,7,8-tetrahydroquinoline-3-carbonitrile and its analogues.

作者信息

Gholap Atul R, Toti Kiran S, Shirazi Fazal, Kumari Ratna, Bhat Manoj Kumar, Deshpande Mukund V, Srinivasan Kumar V

机构信息

Division of Organic Chemistry; Technology, National Chemical Laboratory, Pune, India.

出版信息

Bioorg Med Chem. 2007 Nov 1;15(21):6705-15. doi: 10.1016/j.bmc.2007.08.009. Epub 2007 Aug 15.

DOI:10.1016/j.bmc.2007.08.009
PMID:17765545
Abstract

A series of 2-amino-5-oxo-4-phenyl-5,6,7,8-tetrahydroquinoline-3-carbonitrile and various analogues have been synthesized in excellent isolated yields starting from various arylidenemalononitrile and 3-amino-2-cyclohexen-1-one in 1-propanol as solvent at reflux temperature in the absence of any added catalyst. All the synthesized compounds were evaluated for their antifungal activity. The relationship between functional group variation and biological activity of the evaluated compounds is discussed in the article.

摘要

以各种亚芳基丙二腈和3-氨基-2-环己烯-1-酮为原料，在1-丙醇作为溶剂、回流温度且无任何添加催化剂的条件下，合成了一系列2-氨基-5-氧代-4-苯基-5,6,7,8-四氢喹啉-3-腈及其各种类似物，分离产率优异。对所有合成化合物的抗真菌活性进行了评估。文章讨论了所评估化合物的官能团变化与生物活性之间的关系。

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