氨基乙基-哌嗪-硝基咪唑杂化化合物的设计、合成及抗菌性能评价。

IF 1.8 4区 生物学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences Pub Date : 2023-03-28 DOI:10.1515/znc-2022-0043
Anas J Rasras, Raed A Al-Qawasmeh, Mohamed El-Naggar, Ihsan Shehadi, Mahmoud M Elaasser, Yaseen A Al-Soud
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引用次数: 0

摘要

通过三组分反应制备了一系列新的氨基乙基硝基咪唑哌嗪杂化化合物。在Cu (I)催化剂的作用下,采用曼尼型反应将含丙炔基部分的硝基咪唑与仲胺和甲醛偶联。新合成的分子10a-10w,通过核磁共振和质谱进行了模糊的表征。制备的化合物在体外对选定的革兰氏阳性菌和革兰氏阴性菌进行抑菌活性评价。所有化合物对革兰氏阴性菌的活性均不显著。化合物10m、10q、10s和10t对革兰氏阳性菌金黄色葡萄球菌、枯草芽孢杆菌以及真菌大肠杆菌和普通变形杆菌具有中等活性。
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Design, synthesis and antimicrobial assessments of aminoacetylenic-piperazine nitroimidazole hybrid compounds.

A new series of aminoacetylenic nitroimidazole piperazine hybrid compounds were prepared via three-component reaction. Mannich-type reaction was utilized to couple the nitroimidazole containing propargylic moiety with secondary amines and formaldehyde in the presence of Cu (I) catalyst. The newly synthesized molecules 10a-10w, were characterized an ambiguously through NMR and mass spectrometry. The prepared compounds were assessed in vitro for their antibacterial activity against selected gram-positive and gram-negative bacteria. All of the compounds had shown insignificant activities toward gram-negative bacteria. While compounds 10m, 10q, 10s and 10t had shown moderate activities against the gram-positive bacteria Staphylococcus aureus, Bacillus subtilis and against fungi Escherichia coli and Proteus vulgaris.

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来源期刊
CiteScore
4.10
自引率
5.00%
发文量
55
期刊介绍: A Journal of Biosciences: Zeitschrift für Naturforschung C (ZNC) is an international scientific journal and a community resource for the emerging field of natural and natural-like products. The journal publishes original research on the isolation (including structure elucidation), bio-chemical synthesis and bioactivities of natural products, their biochemistry, pharmacology, biotechnology, and their biological activity and innovative developed computational methods for predicting the structure and/or function of natural products. A Journal of Biosciences: Zeitschrift für Naturforschung C (ZNC) welcomes research papers in fields on the chemistry-biology boundary which address scientific ideas and approaches to generate and understand natural compounds on a molecular level and/or use them to stimulate and manipulate biological processes.
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