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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis of uriedo and thiouriedo derivatives of peptide conjugated heterocycles - A new class of promising antimicrobials.
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Synthesis of uriedo and thiouriedo derivatives of peptide conjugated heterocycles - A new class of promising antimicrobials.

机译:肽共轭杂环的尿素和硫脲衍生物的合成-一种新型的有前途的抗菌剂。

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摘要

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.
机译:通过肽共轭杂环分别与异氰酸酯和异硫氰酸酯反应,合成了四十五种脲和硫脲的新衍生物。所有化合物均已通过IR,(1)H NMR,质量和元素分析进行​​了表征。评价这些化合物抑制一组微生物生长的能力,并且所有合成的化合物均显示出优异的抗微生物活性。从结构-活性关系研究中可以明显看出,硫脲的活性略高于脲。同样,标题化合物的苯环上的取代基在活性中起关键作用。此外,化合物40的效力比所用标准物强近二十倍。这些结果为该领域的进一步研究提供了平台。

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