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Synthesis of new pyrazolone and pyrazole-based adamantyl chalcones and antimicrobial activity.
Bioscience Reports ( IF 4 ) Pub Date : 2020-09-11 , DOI: 10.1042/bsr20201950
Rawan Al-Saheb 1 , Sami Makharza 2 , Feras Al-Battah 3 , Rajab Abu-El-Halawa 4 , Tawfeq Kaimari 2 , Omar S Abu Abed 5
Affiliation  

Chalcones and their derivatives are becoming increasingly popular due to their various pharmacological effects. Chalcone molecules may be extracted from natural resources, entirely synthesised, or biosynthesised by modifying the natural ones. In this study, five pyrazole based adamantyl heterocyclic compounds were synthesised by condensation of 1-adamantyl chalcone with substituted phenylhydrazine. The products were characterised by using ¹HNMR, ¹³CNMR and FT-IR spectroscopy. The microbiological activity of these compounds was investigated against bacteria and fungi. The new compounds showed good to moderate activity against the microbial species used for screening. All developed molecules showed antibacterial activity against gram-negative and gram-positive. These molecules showed antifungal activities against Fusarium oxysporum fungus and in a dose-dependent manner, apart from RS-1 molecules which showed compromised antifungal activity and even at a high dose.

中文翻译:

新型吡唑啉酮和吡唑基金刚烷基查耳酮的合成及其抗菌活性。

查尔酮及其衍生物由于其各种药理作用而变得越来越受欢迎。查耳酮分子可以从天然资源中提取,完全合成或通过修饰天然分子而生物合成。在这项研究中,通过1-金刚烷基查尔酮与取代的苯肼的缩合合成了五种吡唑基的金刚烷基杂环化合物。产物通过1 HNMR,13 CNMR和FT-IR光谱表征。研究了这些化合物对细菌和真菌的微生物活性。新化合物对用于筛选的微生物物种显示出良好至中等的活性。所有已开发的分子均显示出对革兰氏阴性和革兰氏阳性的抗菌活性。
更新日期:2020-09-13
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