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肽缀合杂环的尿苷和硫代尿苷衍生物的合成 - 一类有前途的新型抗菌药物。

Synthesis of uriedo and thiouriedo derivatives of peptide conjugated heterocycles - A new class of promising antimicrobials.

机构信息

Department of Studies in Chemistry, Manasagangotri, University of Mysore, Mysore 570 006, India.

出版信息

Eur J Med Chem. 2012 Feb;48:179-91. doi: 10.1016/j.ejmech.2011.12.012. Epub 2011 Dec 14.

Abstract

Forty five new derivatives of ureas and thioureas were synthesized by the reaction of peptide conjugated heterocycles with isocyanates and isothiocyanates respectively. All the compounds have been characterized by IR, (1)H NMR, mass and elemental analysis. The compounds were evaluated for their ability to inhibit the growth of a panel of microorganisms and all the synthesized compounds displayed an excellent antimicrobial activity. From structure-activity relationship studies, it was apparent that thioureas infact is slightly more active than ureas. Also, substituents on the phenyl ring of the title compounds play a key role in the activity. Further, compound 40 is nearly twenty times more potent than the standard used. These results present a platform for the further studies in this line.

摘要

通过肽共轭杂环与异氰酸酯和异硫氰酸酯的反应,合成了 45 种新的脲和硫脲衍生物。所有化合物均通过 IR、(1)H NMR、质谱和元素分析进行了表征。评估了这些化合物抑制一系列微生物生长的能力,所有合成的化合物均表现出优异的抗菌活性。从构效关系研究中可以看出,硫脲实际上比脲略为活跃。此外,标题化合物苯环上的取代基在活性中起着关键作用。此外,化合物 40 的效力比使用的标准品强近 20 倍。这些结果为进一步研究提供了一个平台。

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