Synthesis and evaluation of some novel chromone based dithiazoles as antimicrobial agents.

International Journal of Medicinal Chemistry Pub Date : 2013-01-01 Epub Date: 2013-11-27 DOI:10.1155/2013/815453
Naureen Aggarwal, Vishal Sharma, Harpreet Kaur, Mohan Paul Singh Ishar
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引用次数: 7

Abstract

Novel substituted 1,2,4-dithiazolylchromones 3a-j were synthesized by the reaction of 3-formylchromones (1a-j) with two equivalents of p-chlorothiobenzamide (2) in dry xylene and characterized spectroscopically (IR, (1)H and (13)C NMR, mass) and elemental analysis. All synthesized compounds were screened for in vitro antimicrobial activity against various pathogenic bacterial and fungal strains and were found to possess good to moderate inhibitory potential against all tested strains. Antimicrobial results reveal that compounds bearing lipophilic electron withdrawing groups such as chloro and bromo displayed significant inhibitory potential against both bacterial and fungal strains. Particularly, compound 3c displayed significant inhibitory against bacterial strains and compound 3h exhibits significant inhibitory potential in comparison to standard drug fluconazole against fungal strain S. cerevisiae.

Abstract Image

新型铬基二噻唑类抗菌药物的合成与评价。
以3-甲酰基chromones (1a-j)与对氯硫苯酰胺(2)在干二甲苯中反应合成了新型取代的1,2,4-二噻唑基chromones 3a-j,并通过IR, (1)H和(13)C NMR,质量和元素分析对其进行了表征。所有合成的化合物对各种病原菌和真菌菌株的体外抗菌活性进行了筛选,发现对所有测试菌株具有良好到中等的抑制潜力。抗菌结果表明,含有亲脂性吸电子基团(如氯和溴)的化合物对细菌和真菌菌株都有显著的抑制潜力。特别是,化合物3c对细菌菌株表现出显著的抑制作用,化合物3h与标准药物氟康唑相比,对酿酒葡萄球菌真菌菌株表现出显著的抑制潜力。
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期刊介绍: International Journal of Medicinal Chemistry is a peer-reviewed, Open Access journal that publishes original research articles as well as review articles in all areas of chemistry associated with drug discovery, design, and synthesis. International Journal of Medicinal Chemistry is a peer-reviewed, Open Access journal that publishes original research articles as well as review articles in all areas of chemistry associated with drug discovery, design, and synthesis.
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