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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Synthesis and biological evaluation of novel (L)-alpha-amino acid methyl ester, heteroalkyl, and aryl substituted 1,4-naphthoquinone derivatives as antifungal and antibacterial agents.
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Synthesis and biological evaluation of novel (L)-alpha-amino acid methyl ester, heteroalkyl, and aryl substituted 1,4-naphthoquinone derivatives as antifungal and antibacterial agents.

机译:新型(L)-α-氨基酸甲酯,杂烷基和芳基取代的1,4-萘醌衍生物作为抗真菌剂和抗菌剂的合成及生物学评估。

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摘要

A series of (S)-N-(1,4-naphthoquinon-2-yl)-alpha-amino acid methyl esters 3-9, 2-N,N-dialkylamino-1,4-naphthoquinones 10-11 and 2-hydroxy-3-(2'-mercaptoimidazolyl)-1,4-naphthoquinones and their cyclic analogs 12-15 were synthesized and evaluated for antifungal and antibacterial activities. The structure-activity relationships of these compounds were studied and the results show that the compounds 9b and 13c exhibited in vitro antifungal activity against Candida albicans, Cryptococcus neoformans, and Sporothrix schenckii, whereas compound 6a showed in vitro antibacterial activity against Streptococcus faecalis, K. pneumoniae, Escherichia coli, and Staphylococcus aureus.
机译:一系列(S)-N-(1,4-萘醌-2-基)-α-氨基酸甲酯3-9,2-N,N-二烷基氨基-1,4-萘醌10-11和2-合成了羟基-3-(2'-巯基咪唑基)-1,4-萘醌及其环状类似物12-15,并评估了其抗真菌和抗菌活性。研究了这些化合物的结构活性关系,结果表明化合物9b和13c对白色念珠菌,新隐球菌和schenothrix schenckii表现出体外抗真菌活性,而化合物6a对粪便链球菌K表现出体外抗菌活性。肺炎,大肠埃希菌和金黄色葡萄球菌。

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