3,6-二取代 1,2,4-三唑并[3,4-b][1,3,4]噻二唑的合成及抗菌活性研究。
Studies on the synthesis and antibacterial activity of 3,6-disubstituted 1,2,4-triazolo[3,4-b]1,3,4-thiadiazoles.
机构信息
Department of Organic Chemistry, Faculty of Pharmacy, Medical University, Chodźki 4a, 20-093 Lublin, Poland.
出版信息
Eur J Med Chem. 2012 Jan;47(1):580-4. doi: 10.1016/j.ejmech.2011.10.055. Epub 2011 Nov 6.
Treating infections caused by drug-resistant bacterial strains constitutes one of the most essential challenges for medicine nowadays. A range of new derivatives of 1,2,4-triazolo[3,4-b]1,3,4-thiadiazole have been synthesized and evaluated for their in vitro antimicrobial activity. Compounds 1-8 indicated high activity towards Gram-positive bacteria, which was up to 16 times more than currently used antibiotics. To the best of our knowledge, the derivatives obtained by us are the most active among the 3-aryl-6-arylamino-1,2,4-triazolo[3,4-b]1,3,4-thiadiazoles known until now.
治疗由耐药菌引起的感染是当今医学最基本的挑战之一。一系列 1,2,4-三唑并[3,4-b]1,3,4-噻二唑的新衍生物已被合成并评估其体外抗菌活性。化合物 1-8 对革兰氏阳性菌表现出高活性，其活性比目前使用的抗生素高 16 倍。据我们所知，我们获得的衍生物是迄今为止已知的 3-芳基-6-芳氨基-1,2,4-三唑并[3,4-b]1,3,4-噻二唑中活性最高的。
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