27623-03-6Relevant articles and documents
Synthesis, biological activity, molecular docking studies of a novel series of 3-Aryl-7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives as the acetylcholinesterase inhibitors
Jin, Zhe,Zhang, Chao,Liu, Miao,Jiao, Simeng,Zhao, Jing,Liu, Xiaoping,Lin, Huangquan,Chi-cheong Wan, David,Hu, Chun
, p. 2478 - 2489 (2021)
The acetylcholinesterase inhibitors play a critical role in the drug therapy for Alzheimer’s disease. In this study, twenty-nine novel 3-aryl-7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives were synthesized and assayed for their human acetylcholinesterase (hAChE) inhibitory activities. Inhibitory ratio values of seventeen compounds were above 55% with 4c having the highest value as 77.19%. The compounds with the halogen atoms in the aromatic ring, and N,N-diethylamino or N,N-dimethylamino groups in the side chains at C-3 positions exhibited good inhibitory activity. SAR study was carried out by means of molecular docking technique. According to molecular docking results, the common interacting site for all compounds were found to be peripheral anionic site whereas highly active compounds were interacting with the catalytic active site too. HIGHLIGHTS A novel series of 3-aryl-7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives were synthesized and assayed for their human acetylcholinesterase (hAChE) inhibitory activities. The SAR study of the target 3-aryl-7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives was summarized. The active sites in the acetylcholinesterase were analyzed by molecular docking technique. Communicated by Ramaswamy H. Sarma.
Thiazole[3,2-b]-1,2,4-thiazole derivatives and application thereof
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Paragraph 0117; 0118, (2018/02/04)
The invention belongs to the technical field of medicine and relates to thiazole[3,2-b]-1,2,4-thiazole derivatives and an application thereof. The thiazole[3,2-b]-1,2,4-thiazole derivatives comprise thiazole[3,2-b]-1,2,4-thiazole derivative compounds as well as stereoisomers and pharmaceutically applicable salts of the compounds, and a general structural formula of the compounds is represented in the specification; the thiazole[3,2-b]-1,2,4-thiazole derivatives and the pharmaceutically applicable acid-addition salts of the compounds can be combined with existing drugs or separately utilized to serve as glucose concentration dependent type insulin secretion accelerants for treatment of type II diabetes. Compared with the prior art, the compounds are the glucose concentration dependent type insulin secretion accelerants, can promote insulin secretion under high glucose concentration and do not influence insulin secretion under low glucose concentration, so that the side effect of hypoglycemia is avoided.
Synthesis and biological evaluation of 3,6-diaryl-7H-thiazolo[3,2-b] [1,2,4]triazin-7-one derivatives as acetylcholinesterase inhibitors
Jin, Zhe,Yang, Liu,Liu, Si-Jie,Wang, Jian,Li, Shuo,Lin, Huang-Quan,Wan, David Chi Cheong,Hu, Chun
experimental part, p. 1641 - 1649 (2011/08/06)
Acetylcholinesterase (AChE) inhibitors played an important role in developing a cure for Alzheimer' s disease. In order to study on the influence of modifications at different groups and side chains on the AChE inhibitory ability and the active sites of 7
Syntheses of Thiazolo- and Thiazinotriazinones
Arndt, Friedrich,Franke, Wilfried,Klose, Walter,Lorenz, Joerg,Schwarz, Katica
, p. 1302 - 1307 (2007/10/02)
The syntheses of the thiazolo- and thiazinotriazinones 3 - 6 are described.Preparations of compounds 3 and 5 were achieved regiospecifically by using the compounds 12 and 13.
