高价碘介导合成作为抗菌剂的1-芳基/杂芳基-1,2,4-三唑并[4,3-a]吡啶和1-芳基/杂芳基5-甲基-1,2,4-三唑并[4,3-a]喹啉
Hypervalent iodine mediated synthesis of 1-aryl/hetryl-1,2,4-triazolo[4,3-a] pyridines and 1-aryl/hetryl 5-methyl-1,2,4-triazolo[4,3-a]quinolines as antibacterial agents.
作者信息
Sadana Anil K, Mirza Yasmin, Aneja Kamal R, Prakash Om
机构信息
Department of Chemistry, Kurukshetra University, Kurukshetra 136119, India.
出版信息
Eur J Med Chem. 2003 May;38(5):533-6. doi: 10.1016/s0223-5234(03)00061-8.
Oxidation of 2-pyridyl and 2-quinylhydrazones with iodobenzene diacetate (IBD) in dichloromethane yield 1-aryl/hetryl-1,2,4-trizolo-[4,3-a] pyridines (3a-f) and 1-aryl/hetryl-5-methyl-1,2,4-triazolo[4,3-a] quinolines (6a-f). Seven compounds were tested in vitro for their antibacterial activity. 1-(5'-Nitro-2-furyl)-5-methyl-1,2,4-triazolo[4,3-a]quinoline (6e) was associated with substantially higher antibacterial activity than some commercial antibiotics against Salmonella typhi at MIC i.e. 10 microg mL(-1).
在二氯甲烷中，用二醋酸碘苯（IBD）氧化2 - 吡啶基腙和2 - 喹啉基腙，生成1 - 芳基/杂芳基 - 1,2,4 - 三唑并[4,3 - a]吡啶（3a - f）和1 - 芳基/杂芳基 - 5 - 甲基 - 1,2,4 - 三唑并[4,3 - a]喹啉（6a - f）。对七种化合物进行了体外抗菌活性测试。1 - （5'-硝基 - 2 - 呋喃基） - 5 - 甲基 - 1,2,4 - 三唑并[4,3 - a]喹啉（6e）在最低抑菌浓度即10微克/毫升（-1）时，与一些市售抗生素相比，对伤寒沙门氏菌具有显著更高的抗菌活性。
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