380560-03-2Relevant academic research and scientific papers
Biological evaluation of halogenated thiazolo[3,2-a]pyrimidin-3-one carboxylic acid derivatives targeting the YycG histidine kinase
Zhao, Dan,Chen, Chen,Liu, Huayong,Zheng, Likang,Tong, Yao,Qu, Di,Han, Shiqing
, p. 500 - 507 (2015/01/09)
With an intention to potent inhibitors of YycG histidine kinase, a series of halogenated thiazolo[3,2-a]pyrimidin-3-one carboxylic acid derivatives were synthesized and evaluated for their antibacterial, antibiofilm and hemolytic activities. The majority of the compounds showed good activity against Staphylococcus epidermidis and Staphylococcus aureus, with MIC values of 1.56-6.25 μM, simultaneously presented promising antiobifilm activity against S. epidermidis ATCC35984 at 50 μM. The test of inhibitory activity on YycG kinase suggested the antibacterial activities of these derivatives are based on inhibiting the enzyme activity of the YycG HK domain. The hemolytic activity test suggested these compounds exhibited in vitro antibacterial activity at non-hemolytic concentrations.
Synthesis and reactions of some new 2,3-dihydro-5H-5,7-diarylthiazolo-[3,2-a]pyrimidine-3-one derivatives and their antibacterial and fungicidal activity
Salama,El-Essa
, p. 173 - 179 (2007/10/03)
Arylmethylene acetophenone derivatives (chalcones) Ia-d react with thiourea in glacial acetic acid CH3COOH/Ac2O in the presence of anhydrous sodium acetate to yield 1,4-dihydro-4,6-diarylpyrimidine-2-thione 2a-d which on treatment with chloroacetic acid furnish 2,3-dihydro-5H-5,7-diaryl thiazolo[3,2-a]pyrimidine-3-one derivatives 3a-d. Compounds 3a-d on condensation with aromatic aldehydes yield 2(arylmethylene)-2,3-dihydro-5H-5,7-diaryl-thiazolo[3,2-a]pyrimidine-3-one derivatives 4a-f. Also compounds 4a-d have been prepared directly from 2a,b by the reaction with chloroacetic acid and the aromatic aldehyde. Coupling of 3a-d with aryl diazonium salts in pyridine yields 2-(aryl hydrazo)-2,3-dihydro-5,7-diaryl- 5H-thiazolo[3,2-a]pyrimidine-3-ones 5a-f. Compounds 2a-d on reaction with 2-bromopropionic or 3-bromopropionic acid give 2,3-dihydro-2-methyl-5H-5,7-diaryl-thiazolo[3,2-a]pyrimidine-3-one 6a-d and 2,3-dihydro-6H-6,8-diaryl-pyrimido- [3,2-b]-1,3-thiazin-4-ones 7a-d respectively. A number of 3,4-dihydro-4,6-diaryl pyrimidine-2yl-thio)acetahydrazide 8a-c, 2-(3,4-dihydro-4,6-d[aryl-pyrimidine-2yl-thio)acetanilide derivatives 8d-g, 2-(3,4-dihydro-4,6-diaryl-pyrimidine-2yl-thio)- propionylhydrazide 9a-c, 2-(3,4-dihydro-4,6-diaryl-pyrimidine-2yl-thio)propionylanilide 9d-f and 3-(3,4-dihydro-4,6-diaryipyrimidine-2yl-thio)propionamide 10a-e derivatives are readily obtained in good yield by the action of the corresponding amines on compounds 3, 6 or 7 successively. The anilide 8d also has been obtained by the reaction of compound 2a with chloroacetanilide.
