143700-71-4Relevant 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; 0068, (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, crystal structure and biological evaluation of some novel 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles and 1,2,4-triazolo[3,4-b]-1,3,4- thiadiazines
Khan, Imtiaz,Zaib, Sumera,Ibrar, Aliya,Rama, Nasim Hasan,Simpson, Jim,Iqbal, Jamshed
, p. 167 - 177 (2014/04/17)
Nitrogen-containing heterocycles are of particular interest and significant importance for the discovery of potent bioactive agents in pharmaceutical industry. The present study reports the synthesis of a library of new conjugated heterocycles including 3,6-disubstituted-1,2,4-triazolo-[3,4-b]-1,3,4- thiadiazoles (4a-g and 5a-e) and 3,6-disubstituted-1,2,4-triazolo-[3,4-b]-1,3,4- thiadiazines (6a-h), by cyclocondensation reaction of 4-amino-5-(pyridin-4-yl)- 4H-1,2,4-triazole-3-thiol 3 with various substituted aromatic acids and phenacyl bromides, respectively. The structures of newly synthesized compounds were characterized by elemental analysis, IR, 1H and 13C NMR spectroscopy and in case of 4c by X-ray crystallographic analysis. Newly synthesized triazolothiadiazoles and thiadiazines were screened for acetyl- and butyryl-cholinesterases and alkaline phosphatase inhibition. Almost all of the compounds showed good to excellent activities against acetylcholinesterase more than the reference drugs. Compound 5d exhibited IC50 value 0.77 ± 0.08 μM against acetylcholinesterase and 4a showed IC50 9.57 ± 1.42 μM against butyrylcholinesterase. Among all the tested compounds, 4a also proved as excellent inhibitor of alkaline phosphatase with IC50 0.92 ± 0.03 μM. These heteroaromatic hybrid structures were also tested for their anticancer activity against lung carcinoma (H157) and kidney fibroblast (BHK-21) cell lines and leishmanias. Variable cell growth inhibitory activities were obtained and many compounds exhibit potent %inhibition.
Synthesis and biological activity test of some new five membered heterocycles
Xia, Qingchun,Xu, Dongfang,He, Qizhuang,Li, Xingyu,Sun, Dazhi
, p. 2433 - 2440 (2011/10/05)
A new series of 1,3,4-oxadiazoles, 1,2,4-triazoles, 1,3,4-thiadiazoles were synthesized using alkylhydrazides as the starting materials, and then 1,2,4-triazoles were used to synthesize [1,2,4]triazolo[3,4-b][1,3,4] thiadiazoles. All the compounds were evaluated for in vitro antibacterial activity and antitumor activity. A new series of five membered heterocyclic compounds were synthesized using alkylhydrazides as the starting materials. All the compounds were evaluated for in vitro antibacterial activity and antitumor activity.
