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1,2,3-三取代-1,4-二氢苯并[g]喹喔啉-5,10-二酮及相关化合物作为抗真菌和抗菌剂的设计、合成与生物学评价

Design, synthesis, and biological evaluation of 1,2,3-trisubstituted-1,4-dihydrobenzo[g]quinoxaline-5,10-diones and related compounds as antifungal and antibacterial agents.

作者信息

Tandon Vishnu K, Yadav Dharmendra B, Maurya Hardesh K, Chaturvedi Ashok K, Shukla Praveen K

机构信息

Department of Chemistry, University of Lucknow, Lucknow 226007, India.

出版信息

Bioorg Med Chem. 2006 Sep 1;14(17):6120-6. doi: 10.1016/j.bmc.2006.04.029. Epub 2006 Jun 27.

DOI:10.1016/j.bmc.2006.04.029
PMID:16806945
Abstract

A series of (S)-N-(3-chloro-1,4-naphthoquinon-2-yl)-alpha-amino acid ethyl esters 3 and 1,2,3-trisubstituted-1,4-dihydrobenzo[g]quinoxaline-5,10-diones 6-23 were synthesized and evaluated for antifungal and antibacterial activities. The structure-activity relationship of these compounds was studied and the results show that the compounds 3a and 3b exhibited in vitro antifungal activity against Candida albicans, Cryptococcus neoformans, and Sporothrix schenckii whereas compounds 12 and 22 showed in vitro antibacterial activity against Klebsiella pneumoniae and Escherichia coli.

摘要

合成了一系列(S)-N-(3-氯-1,4-萘醌-2-基)-α-氨基酸乙酯3以及1,2,3-三取代-1,4-二氢苯并[g]喹喔啉-5,10-二酮6 - 23,并对其抗真菌和抗菌活性进行了评估。研究了这些化合物的构效关系,结果表明化合物3a和3b对白色念珠菌、新型隐球菌和申克孢子丝菌具有体外抗真菌活性,而化合物12和22对肺炎克雷伯菌和大肠杆菌具有体外抗菌活性。

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