181058-43-5Relevant articles and documents
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 and radiation stability of novel thiazolopyrimidines with expected antifungal activity
Ghorab,Mohamed,Mohamed,Ammar
, p. 249 - 256 (2007/10/03)
A number of thiazolopyrimidines (II-VII) were prepared through interaction of 6-methyl-4(4′-chlorophenyl)-2-thioxo-1,2,3,4-tetrahydropyrimidine-5- carboxylic acid ethyl ester (Ia) with many reagents. The antifungal activity of all prepared compounds have been determined using Dithane M-45 as a standard fungicide. Some compounds showed a high fungicidal activity equivalent to that of the standard towards Aspergillus niger and Aspergillus ochraceus. Also some biologically active compounds were subjected to gamma irradiation and the structures are stable.