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3-(4-哌嗪-1-苯基)-6-取代-s-三唑并[3,4-b][1,3,4]噻二唑盐酸盐的合成及抗菌活性 被引量:11

Synthesis and antibacterial activity of 3-(4-piperazin-1-yl-phenyl)-s-triazolo[3,4-b][1,3,4] thiadiazole hydrochlorides
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摘要 为了研究水溶性稠杂环化合物的合成方法及抗菌活性,本研究采用3-(4-氯苯基)-6-取代-s-三唑并[3,4-b][1,3,4]噻二唑(2a^n)在相转移催化剂TBAI作用下与哌嗪发生亲核取代,再与盐酸成盐制备了3-(4-哌嗪-1-苯基)-6-取代-s-三唑[3,4-b][1,3,4]噻二唑盐酸盐(3a^n)。用试管二倍稀释法研究了新化合物的体外抗菌活性。结果表明,合成的28个新化合物极性碱性哌嗪基的引入可提高化合物的抗菌活性。该类稠杂环化合物的结构有待进一步优化。 To study the synthetic method and antibacterial activity of water-soluble fused heterocyclic compounds containing piperazine group, the nucleophilic substitution of 3-(4-chlorophenyl)-6-substituteds-triazolo- [ 3,4-b ] [ 1,3,4 ] thiadiazoles (2a - n) with piperazine in the presence of phase transfer catalyst TBAI afforded 3-(4-piperazin-1 -yl-phenyl) -6-substituted-s-triazolo [ 3,4-b ] [ 1,3,4 ] thiadiazole and then followed by acid treatment afforded 3- ( 4-piperazin-1 -yl-phenyl ) -6-substituted-s-triazolo [ 3,4-b ] [ 1,3,4 ] thiadiazole hydrochlorides (3a- n). Twenty-eight new compounds were synthesized and their structures were confirmed by IR, i H NMR, MS and element analysis. The in vitro antibacterial activities of all newly synthesized compounds were tested against Gram positive bacteria and Gram negative bacteria with the standard 2-fold agar dilution method. Fourteen title compounds exhibited potential antibacterial activities in vitro. The structures of these compounds needed to be further optimized.
出处 《药学学报》 CAS CSCD 北大核心 2007年第1期54-57,共4页 Acta Pharmaceutica Sinica
基金 国家自然科学基金资助项目(30070861) 河南大学科研基金资助项目(04ZDZR009).
关键词 相转移催化剂 均三唑并噻二唑 抗菌活性 phase transfer catalyst s-triazolo be further optimized.
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  • 1张自义,张艳,惠新平,许鹏飞,沈大鹏.肼类衍生物在五元唑类杂环合成中的应用进展[J].有机化学,2004,24(11):1348-1365. 被引量:22
  • 2汪敦佳.盐酸环丙沙星合成工艺的改进[J].中国医药工业杂志,1994,25(7):296-298. 被引量:20
  • 3Wang Z Y,药学学报,1999年,34卷,2期,151页
  • 4Zhang Z Y,有机化学,1986年,6卷,3期,184页
  • 5Byrskier A. Novelties in the field of fluoroquinolone [J]. Exp Open Invest Drugs, 1997,6(8):1227-1231.
  • 6Chen YL, Fang KC, Sheu JY, et al. Synthesis and antibacterial evaluation of certain quinolone derivatives [J]. J Med Chem, 2001,44(14):2374-2377.
  • 7Chu DTW, Plattner JJ, Katz L. New directions antibacterial research [J]. J Med Chem, 1996,39(20):3874-3878.
  • 8Kondo H, Sakamoto F, Kawakami K, et al. Studies on prodrugs, 7. Synthesis and antimicrobial activity of 3-formylquinolone derivatives [J]. J Med Chem, 1988,31(1):221-227.
  • 9Bryskier A, Chantot JF. Classification and structure activity relationships of fluoroquinolone [C]. Drugs, 1995,(Suppl 2):16-18.
  • 10(a) Hu, G. Q.; Huang, W. L.; Zhang, H. B.; Huang, S. T.; Wang, H. Chin. J. Chem. 2002, 20, 1115. (b) Hu, G. Q.; Huang, W. L.; Zhang, H. B.; Huang, S. T.; Wang, H. Chin. J. Org. Chem. 2002, 22, 667 (in Chinese).(胡国强, 黄文龙, 张惠斌, 黄胜堂, 汪海, 有机化

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