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雷夫康唑的杂种:合成与生物评价。

Hybrids of ravuconazole: synthesis and biological evaluation.

机构信息

Department of Chemistry, K.T.H.M. College, Nashik 422005, India.

出版信息

Eur J Med Chem. 2012 Aug;54:295-302. doi: 10.1016/j.ejmech.2012.05.010. Epub 2012 May 15.

Abstract

In continuation of our work on antimicrobial agents, a number of hybrid molecules 4a-y containing thiazole and triazole pharmacophores were designed and synthesized. The structure of the compounds was established by IR, NMR, MS and CHN analysis. All the synthesized compounds were tested for qualitative (Zone of inhibition) and quantitative (MIC) antimicrobial activities against four pathogenic bacteria Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa and two pathogenic fungi Candida albicans and Aspergillus niger. Of all the synthesized compounds screened, most of them show potent antimicrobial activity against Gram positive and Gram negative bacteria as well as the fungi species.

摘要

在我们对抗菌药物的研究工作的延续中,设计并合成了一系列含有噻唑和三唑药效团的杂化分子 4a-y。通过红外光谱(IR)、核磁共振(NMR)、质谱(MS)和元素分析(CHN)对化合物的结构进行了确证。对所有合成的化合物进行了定性(抑菌圈)和定量(MIC)抗四种致病菌(枯草芽孢杆菌、金黄色葡萄球菌、大肠杆菌和铜绿假单胞菌)和两种致病真菌(白色念珠菌和黑曲霉)的抗菌活性测试。在所筛选的所有合成化合物中,大多数化合物对革兰氏阳性和革兰氏阴性细菌以及真菌物种表现出很强的抗菌活性。

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