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SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF NEW SUBSTITUTED AZETIDINONYL INDOLYLTRIAZOLE DERIVATIVES

机译:新型取代的氮杂环丁烯基吲哚基三唑衍生物的合成及抗菌活性

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摘要

Cyclocondensation of 4-[2'-substituted alkyl/aryl-5'-methoxy-3'-indolylideno]-3-ethanethioat-5-(substituted phenyl)-1,2,4-triazoles (3a-3h) and 4-[2'-substituted alkyl/aryl-5'-methoxy-3'-indolylideno]-3-benzothioat-5-(substituted phenyl)-1,2,4-triazoles (4a-4h) with chloroacetyl chloride give 4-[3'-chloro-2"-(2-substJtuted alkyl/aryl-5'-methoxy-3'-indolylideno)-4"-oxoazetidinyl]-3-ethanethioat-5-(substituted phenyl)-1,2,4-triazoles (5a-5h) and 4-[3"-chloro-2"-(2-substituted alkyl/ary1-5-methoxy-3'-indolylideno)-4"-oxoazetidinyl]-3-benzothioat-5-(substituted phenyl)-1,2,4-triazoles (6a-6h) respectively. All the synthesized compounds were screened for their antibacterial activity and compared with reference drugs ciprofloxacin and gattifloxacin. The compound 5h was the most potent compound of this series. This compound exhibited promising antibacterial activity against S. aureus (26mm), E. coli (24mm), P. vulgaris (22mm) and K. pneumoniae (23mm). Structure of all the synthesized compounds have been characterized by elemental (C, H, N) and spectral (IR and ~1HNMR) analysis.
机译:4- [2'-取代的烷基/芳基-5'-甲氧基-3'-吲哚基] -3-乙烷硫基-5-(取代的苯基)-1,2,4-三唑(3a-3h)和4-的环缩合用氯乙酰氯将[2'-取代的烷基/芳基-5'-甲氧基-3'-吲哚基] -3-苯甲硫基-5-(取代的苯基)-1,2,4-三唑(4a-4h)得到4- [ 3′-氯-2″-(2-被取代的烷基/芳基-5′-甲氧基-3′-二亚吲哚基)-4″-氧杂氮杂环丁烷基] -3-乙硫基-5-(取代的苯基)-1,2,4-三唑(5a-5h)和4- [3“-氯-2”-(2-取代的烷基/ ary1-5-甲氧基-3'-吲哚亚基)-4“-氧杂氮杂环丁烷基] -3-苯甲硫基-5-(取代分别筛选苯基)-1,2,4-三唑(6a-6h)的所有化合物,并与参考药物环丙沙星和加替沙星比较,化合物5h是该系列中最有效的化合物。具有对金黄色葡萄球菌(26mm),大肠杆菌(24mm),寻常型毕赤酵母(22mm)和肺炎克雷伯氏菌(23mm)的有希望的抗菌活性。通过元素(C,H,N)和光谱(IR和〜1HNMR)分析对其进行了表征。

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