微波诱导氟醌支架一锅Ugi多组分反应的生物学评价

IF 1.1 Q3 CHEMISTRY, MULTIDISCIPLINARY Current Green Chemistry Pub Date : 2020-12-24 DOI:10.2174/2213346107999201224110618
N. Patel, R. Parmar, Hetal I. Soni
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引用次数: 0

摘要

本文介绍了一系列新型氟喹诺酮支架的微波辐射一锅Ugi多组分反应的简便有效工艺。在此基础上,设计了一种新的合成这种特权支架的路线,该路线具有更高的产率、简洁的程序、高效的时间和简单的操作。我们的目的是通过微波诱导的一锅Ugi多组分反应开发具有生物活性的氟喹诺酮支架。通过IR、1H NMR、13C NMR和质谱对所有合成的分子进行了表征。合成的化合物对两种革兰氏阴性菌(大肠杆菌、铜绿假单胞菌)、两种革兰氏阳性菌(葡萄球菌、化脓性链球菌)、,和三种真菌(白色念珠菌、黑曲霉、Aspergillusclavatus)利用MIC(最小抑制浓度)法和抗结核活性H37Rv利用L.J.Slope法。这些新衍生物中的一些表现出中等的良好体外抗菌、抗真菌和抗结核活性。
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Microwave Induced One Pot Ugi Multicomponent Reaction of Fluoroquino Lone Scaffolds: Their Biological Evaluation
Microwave irradiated facile and efficient process for one pot Ugi multicomponent reaction of a novel series of fluoroquinolone scaffolds is described here. On the basis of this approach, a new route to synthesize this privileged scaffolds was designed with higher yields, a clean procedure, time efficient and simple work-up. Our aim is to develop a biologically active fluoroquinolone scaffolds by microwave induced one pot Ugi multicomponent reaction. All the synthesized molecules were characterized by IR, 1H NMR, 13C NMR, and Mass spectra. The antimicrobial activity of the synthesized compounds was screened against two Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa), two Gram-positive bacteria (Staphylococcus aureus, Streptococcus pyogenes), and three fungi (Candida albicans, Aspergillus niger, Aspergillus clavatus) utilizing the MIC (Minimal Inhibitory Concentration) method and antitubercular activity H37Rv utilizing L. J. Slope method. Some of these novel derivatives demonstrate moderate to good in vitro antibacterial, antifungal and antitubercular activities.
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来源期刊
Current Green Chemistry
Current Green Chemistry CHEMISTRY, MULTIDISCIPLINARY-
CiteScore
4.30
自引率
13.60%
发文量
6
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