7338-80-9Relevant articles and documents
2H-thiazolo [3, 2-b]-1, 2, 4-triazine-3, 7-diketone derivative and application thereof
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, (2020/12/29)
The invention discloses a 2Hthiazolo [3, 2b] 1, 2, 4triazine 3, 7diketone derivative as shown in a general formula I or pharmaceutically acceptable hydrate and salt thereof, the 2Hthiazolo [3, 2b] 1,2, 4triazine 3, 7diketone derivative comprises stereoisomers or tautomers thereof, and R1 and R2 in the general formula I can be optionally selected from one, two or three independently selected fromhydrogen, alkyl, alkoxy, halogen, hydroxyl, acetyl, propionyl, nitro or trifluoromethyl. The 1, 2, 4-triazine 3, 7diketone derivative has an obvious inhibiting effect on acetylcholin esterase, and isused for enhancing the memory of a patient suffering from dementia and Alzheimer's disease. The invention also relates to a preparation method of the compound and the application of the compound in preparation of drugs for treating Alzheimer's disease.
Thiazole[3,2-b]-1,2,4-thiazole derivatives and application thereof
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, (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.
Design, synthesis, and biological evaluation of 7H-thiazolo[3,2-b]-1,2,4- triazin-7-one derivatives as dual binding site acetylcholinesterase inhibitors
Liu, Si-Jie,Cui, Li-Bo,Xu, Hui-Lan,Wang, Tie-Ying,Hu, Chun,Li, Shuo,Lin, Huang-Quan,Wan, David Chicheong
, p. 2607 - 2614 (2014/01/06)
A series of 7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives were designed, synthesized and evaluated as dual binding site acetylcholinesterase inhibitors. The target compounds exhibited promising inhibitory activity for AChE. The structure-activity relationships were discussed and their binding conformation and simultaneous interactions mode were further clarified by the molecular docking studies.
