511309-24-3Relevant 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
supporting information, 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, antimicrobial and DFT studies of novel fused thiazolopyrimidine derivatives
Gupta, Richa,Chaudhary, Ram Pal
, p. 207 - 214 (2013/09/02)
The reaction of dihydropyrimidine-2(1H)-thione 4, obtained by the condensation of chalcone 3 with thiourea, with chloroacetic acid and 1,2-dibromoethane furnished compounds 5 and 6 and not their respective isomers 8 and 9. The regiochemistry of the cycliz
