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新型 N-芳基马来酰亚胺衍生物与α-羟膦酸酯的合成及生物评价。

Synthesis and biological evaluation of novel N-aryl maleimide derivatives clubbed with α-hydroxyphosphonates.

机构信息

Organic Chemistry Research Centre, Department of Chemistry, K.R.T. Arts, B.H. Commerce and A.M. Science College, Gangapur Road, Nashik 422 002, MS, India.

Organic Chemistry Research Centre, Department of Chemistry, K.R.T. Arts, B.H. Commerce and A.M. Science College, Gangapur Road, Nashik 422 002, MS, India.

出版信息

Eur J Med Chem. 2014 Aug 18;83:490-7. doi: 10.1016/j.ejmech.2014.06.053. Epub 2014 Jun 26.

DOI:10.1016/j.ejmech.2014.06.053
PMID:24992076
Abstract

A series of novel molecules 5a-g containing N-aryl maleimide and α-hydroxyphosphonate moieties were synthesized. A distinct approach for high-yielding synthesis of α-hydroxyphosphonates has been discovered using various catalyst and solvents. The structures of the synthesized compounds were elucidated by IR, NMR, MS and CHN analysis. All the synthesized compounds were tested for qualitative (Zone of inhibition) and quantitative (MIC) antimicrobial activities against two pathogenic bacteria such as Bacillus subtilis (NCIM 2250) and Escherichia coli (ATCC 25922) and four pathogenic fungi such as Candida albicans (MTCC 277), Candida tropicalis (MTCC184), Aspergillus niger (MCIM 545) and Aspergillus clavatus (MTCC 132). The investigation of antimicrobial screening data revealed that most of the tested compounds are moderate to good microbial inhibitors.

摘要

一系列新型分子 5a-g 含有 N-芳基马来酰亚胺和 α-羟膦酸酯部分。已经发现了一种使用各种催化剂和溶剂高产率合成 α-羟膦酸酯的独特方法。通过 IR、NMR、MS 和 CHN 分析阐明了合成化合物的结构。所有合成的化合物都进行了定性(抑菌区)和定量(MIC)抗菌活性测试,以评估其对两种病原菌,如枯草芽孢杆菌(NCIM 2250)和大肠杆菌(ATCC 25922)以及四种病原菌真菌,如白色念珠菌(MTCC 277)、热带念珠菌(MTCC184)、黑曲霉(MCIM 545)和棒曲霉(MTCC 132)的抑制作用。抗菌筛选数据的研究表明,大多数测试化合物对微生物具有中等至良好的抑制作用。

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