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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。
In order to study the synthetic methods and antibacterial activities of water-soluble fused heterocyclic compounds, this study used 3- (4-chlorophenyl) -6-substituted-s-triazolo [3,4- b] ] Thiadiazole (2a ~ n) was substituted with piperazine under the action of phase transfer catalyst TBAI and then salified with hydrochloric acid to prepare 3- (4-piperazin-1-phenyl) -triazole [3,4-b] [1,3,4] thiadiazole hydrochloride (3a-n). The in vitro antibacterial activity of the new compounds was studied by two-fold dilution in vitro. The results showed that the synthesis of 28 new compounds with polar basic piperazinyl introduction can improve the antibacterial activity of the compounds. The structure of this class of heterocyclic compounds needs to be further optimized.