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某些稠合杂环[1,2,4]三唑并[3,4-b][1,3,4]噻二唑衍生物的合成与抗菌评价。

Synthesis and antimicrobial evaluation of some fused heterocyclic [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives.

机构信息

Organic Chemistry Department, Faculty of Pharmacy, Traian Vuia Street 6, Bucharest 020956, Romania.

出版信息

Eur J Med Chem. 2010 Dec;45(12):6139-46. doi: 10.1016/j.ejmech.2010.10.007. Epub 2010 Oct 15.

DOI:10.1016/j.ejmech.2010.10.007
PMID:21036422
Abstract

A series of fused 1,2,4-triazoles with diphenylsulfone moiety are prepared utilizing 4-amino-5-[4-(4-X-phenylsulfonyl)phenyl]-4H-1,2,4-triazole-3-thiol 1 (X=H, Br). The latter on reaction with aromatic isothiocyanate in DMF, aromatic acid in POCl3 and CDI in dioxane gives five membered fused triazole derivatives 2a-c, 3a-c, 4a-g, 5a-g and 6a,b. The structures of newly synthesized compounds were confirmed on the basis of their elemental analysis and spectral data results (IR, 1H-and 13C NMR). New synthesized compounds were screened for their antimicrobial activities. The preliminary results revealed that some of the compounds exhibited promising antimicrobial activities.

摘要

利用 4-氨基-5-[4-(4-X-苯磺酰基)苯基]-4H-1,2,4-三唑-3-硫醇 1（X=H，Br）制备了一系列带有二苯砜部分的稠合 1,2,4-三唑。后者与 DMF 中的芳基异硫氰酸酯、POCl3 中的芳基酸和二异丙基碳二亚胺在二氧六环中反应，得到五元稠合三唑衍生物 2a-c、3a-c、4a-g、5a-g 和 6a，b。根据元素分析和光谱数据（IR、1H 和 13C NMR）结果，确定了新合成化合物的结构。新合成的化合物进行了抗菌活性筛选。初步结果表明，一些化合物表现出有希望的抗菌活性。

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