Facile Synthesis, Characterization, and In Vitro Antimicrobial Screening of a New Series of 2,4,6-Trisubstituted-s-triazine Based Compounds.

International Journal of Medicinal Chemistry Pub Date : 2015-01-01 Epub Date: 2015-01-31 DOI:10.1155/2015/571836

Ravi Bhushan Singh, Nirupam Das, Md Kamaruz Zaman

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引用次数: 1

Abstract

A series of new 2,4,6-trisubstituted-s-triazine was synthesized, assessed for antimicrobial activity, and characterized by FTIR, (1)HNMR, (13)CNMR, and elemental analysis. The tested compounds, 4d, 4g, 4h, 4k, and 4n, have shown considerable in vitro antibacterial efficacy with reference to the standard drug ciprofloxacin (MIC 3.125 μgmL(-1) against B. subtilis, E. coli, and K. pneumoniae). It was observed that compounds 4d and 4h displayed equipotent antibacterial efficacy against B. subtilis (MIC 3.125 μgmL(-1)) and S. aureus (MIC 6.25 μgmL(-1)). The studies demonstrated that the para-fluorophenylpiperazine substituted s-triazine (4n) was potent and exhibited broad spectrum antibacterial activity against S. epidermidis, K. pneumoniae, and P. aeruginosa with MIC of 6.25 μgmL(-1) and for E. coli, it showed an MIC of 3.125 μgmL(-1) equipotent with reference to the standard drug. Among all the compounds under investigation, compound 4g also demonstrated significant antifungal activity (3.125 μgmL(-1)) against C. albicans.

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2,4,6-三取代-s-三嗪类化合物的简单合成、表征及体外抗菌筛选

合成了一系列新的2,4,6-三取代-s-三嗪，对其抗菌活性进行了评价，并通过FTIR、(1)HNMR、(13)CNMR和元素分析对其进行了表征。对照标准药环丙沙星(MIC为3.125 μgmL(-1))对枯草芽孢杆菌、大肠杆菌和肺炎克雷伯菌的抑菌效果，所测化合物4d、4g、4h、4k和4n均有较好的体外抑菌效果。结果表明，化合物4d和4h对枯草芽孢杆菌(MIC为3.125 μgmL(-1))和金黄色葡萄球菌(MIC为6.25 μgmL(-1))的抑菌效果相当。研究表明，对氟苯哌嗪取代的s-三嗪(4n)对表皮葡萄球菌、肺炎克氏菌和铜绿假单胞菌具有广谱抗菌活性，MIC值为6.25 μgmL(-1)，对大肠杆菌的MIC值为3.125 μgmL(-1)。在所研究的化合物中，化合物4g对白色念珠菌也表现出显著的抗真菌活性(3.125 μgmL(-1))。

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International Journal of Medicinal Chemistry CHEMISTRY, MEDICINAL-

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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.