76259-22-8Relevant academic research and scientific papers
Thiazole triazole-6-acetamide derivative and application
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, (2018/03/01)
The invention discloses a thiazole [3,2-b] [1,2,4]-triazole-6-acetamide derivative as shown in formula I or a pharmaceutically acceptable hydrate and salt thereof. The derivative comprises a stereisomer or tautomer thereof; R1 in the formula I is hydrogen, methyl, halogen, hydroxy, methoxy group, acetyl, propionyl, nitro or alkoxy; R2 and R3 are independently selected from C1-C6 alkyl or R2 and R3 and nitrogen atoms connected with the R2 and R3 are formed into pyrryl, piperidyl, morpholinyl, N-methyl piperazine and N-phenylpiperazine. The thiazole [3,2-b] [1,2,4]-triazole-6-acetamide derivative disclosed by the invention has an obvious restraining function to acetylcholin esterase and is used for enhancing the memory of the patients suffering from dementia and Alzheimer's disease. The invention also relates to a preparation method of the compound and application of the compound for preparing the drug for treating the senile dementia.
Design and synthesis of some thiazolotriazolyl esters as anti-inflammatory and analgesic agents
Tozkoparan, Birsen,Aytac, S. Peri,Guersoy, Sule,Aktay, Goeknur
, p. 192 - 201 (2012/09/08)
In order to develop potent analgesic/antiinflammatory compounds with reduced ulcerogenic risk, a series of thiazolotriazolyl-carboxylic and acetic acid esters were synthesized and characterized by spectral and elementary analysis. All synthesized compounds were screened for in vivo anti-inflammatory activities in mice by carregeenan-induced paw edema model. The compounds showing 20% reduction in paw edema were also evaluated for their analgesic activities by acetic acid-induced writhing test and the gastric ulceration risk by determining the lipid peroxidation level in stomachs. Among the compounds tested, compounds 1, 4, 6, 7, 8, 1a, 2a, 3a, 4a, 7a, 2b, and 8b showed moderate-to-good anti-inflammatory activity at various doses in any of the measurement intervals. Compounds 7a, 2b, and 8b were the most actives of the series in analgesic activity test. Moreover, compounds 1, 4, and 8 were found to be safe in stomach in respect of free radical production. Springer Science+Business Media, LLC 2010.
Sur la synthese d'acides thiazolotriazolylacetiques
Moskowitz, H.,Mignot, A.,Miocque, M.
, p. 1321 - 1323 (2007/10/02)
During the synthesis of thiazolotriazolylacetic acids, the condensation of ethyl 4-chloro-3-oxobutyrate with triazolinethiones was studied.The use of an alkaline reagent (triethylamine) leads only to S-alkylation and not to the expected cyclized product.T
