113486-84-3Relevant articles and documents
3. 6 - Disubstituted [1, 2, 4] triazolo [3, 4 - b] [1, 3, 4] thiadiazole compound and use thereof
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Paragraph 0052; 0060; 0066, (2018/11/22)
The invention discloses 3,6-disubstituted[1,2,4]triazolyl[3,4-b][1,3,4]thiadiazole compounds represented by general formula (I), and pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof. The compounds can be used as a transpeptidase SrtA inhibitor of Staphylococcus aureus, Bacillus pyogenes, Bacillus anthracis, Streptococcus pneumoniae and other Gram-positive bacteria, and can be used to prepare drugs for treating pathogen infection diseases with the transpeptidase SrtA of the Gram-positive bacteria, such as Staphylococcus aureus, Bacillus pyogenes, Bacillus anthracis and Streptococcus pneumoniae as target. The compounds avoid selection pressure induced drug resistance of pathogens to a certain degree, and mitigate threat of continuous drug-resistant pathogens to the health of human.
Synthesis of Heterocycles. Part VII . Synthesis and Antimicrobial Activity of Some 7H-s-Triazolothiadiazine and s-Triazolothiadiazole Derivatives
Eweiss, N. F.,Bahajaj, A. A.
, p. 1173 - 1182 (2007/10/02)
The cyclization of 4-amino-5-aryl-3-cyanomethylthio-1,2,4-triazoles II in the presence of concentrated sulfuric acid yields 7H-6-amino-s-triazolothiadiazines III.Cyclization of 4-amino-5-aryl-1,2,4-triazole-3-thiones I with phenacyl chloride yields 7H-3-aryl-6-phenyl-s-triazolothiadiazines IV.Similarly, compounds I condensed with cyanogen bromide, phenyl isothiocyanate and carbon disulfide to give the corresponding cyclized products 6-amino-3-aryl-s-triazolothiadiazoles V, 3-aryl-6-phenylamino-s-triazolothiadiazoles VI and 3-aryl-s-triazolothiadiazol-6(5H)thiones VII, respectively.Also in the presence of phosphoryl chloride, compounds I underwent cyclization with monocarboxylic acids and oxalic acid to 3,6-diaryl-s-triazolothiadiazole VIII and 6,6'-bis(3-aryl-s-triazolothiadiazoles) IX.The above compounds were screened for their antimicrobial activity.