Synthesis and study of 1,3,5-triazine based thiazole derivatives as antimicrobial agents

Synthesis and study of 1,3,5-triazine based thiazole derivatives as antimicrobial agents
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DOI:
10.1016/j.jscs.2012.12.004
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发表时间:
2016-09-01
影响因子:
5.6
通讯作者:
Rajpara, K. M.
Rajpara, K. M.
中科院分区:
化学2区
文献类型:
--
作者:
Desai, N. C.;Makwana, Atul H.;Rajpara, K. M.

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通过一系列多步反应合成了一系列新化合物N′-(4-(芳基氨基)-6-(噻唑-2-基氨基)-1,3,5-三嗪-2-基)异烟碱肼(3a-l)。新合成的化合物通过IR、H-1 NMR、C-13 NMR和质谱数据进行了表征。采用连续肉汤稀释法对标题化合物(3a-l)进行革兰氏阳性菌(金黄色葡萄球菌、化脓性链球菌)、革兰氏阴性菌(大肠杆菌、铜绿假单胞菌)和3种真菌(白色念珠菌、黑曲霉、棒曲霉)的抑菌筛选。合成的化合物对试验生物有较强的抑制作用。筛选到的化合物3k和31具有比市售抗生素更高的抗菌和抗真菌活性。(C) 2012年由爱思唯尔B.V.代表沙特国王大学制作和主办。这是一篇基于CC BY-NC-ND许可(http://creativecommons.org/licenses/by-nc-nd/4.0/)的开放获取文章。
A series of novel compounds N'-(4-(arylamino)-6-(thiazol-2-ylamino)-1,3,5-triazin-2-yl)isonicotinohydrazides (3a-l) were synthesized by a series of multistep reactions. Newly synthesized compounds have been characterized by IR, H-1 NMR, C-13 NMR and mass spectral data. Antimicrobial screening of title compounds (3a-l) was examined against Gram-positive bacteria (Staphylococcus aureus, Streptococcus pyogenes), Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa) and three fungi (Candida albicans, Aspergillus niger, Aspergillus clavatus) by using serial broth dilution method. Synthesized compounds showed potent inhibitory action against test organisms. Screened compounds 3k and 3l were associated with considerably higher antibacterial and antifungal activities than commercially used antibiotics. (C) 2012 Production and hosting by Elsevier B.V. on behalf of King Saud University. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).