432533-45-4Relevant articles and documents
Design and discovery of Novel Thiazole acetamide derivatives as anticholinesterase agent for possible role in the management of Alzheimer's
Sun, Zhi-Qing,Tu, Li-Xiang,Zhuo, Feng-Juan,Liu, Song-Xia
supporting information, p. 747 - 750 (2016/05/24)
A novel series of thiazole acetamides was synthesized in excellent yields and characterized with the aid of various spectroscopic and elemental analysis. These compounds were evaluated for in vitro acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities for possible benefit in Alzheimers disease (AD). Among the synthesized compound, 6d was identified as the most potent compound of AChE (IC50= 3.14 ± 0.16 μM) with a selectivity index (SI) of 2.94 against BuChE. These compounds were further tested for inhibition of Aβ aggregation and β-secretase, where it showed potent inhibition which confirmed its multifactorial benefits in AD. The toxicity and docking study were also carried out to exemplify the pharmacological profile of compound 6d as prospective lead molecule against AD.
Design and synthesis of thiazole derivatives as potent FabH inhibitors with antibacterial activity
Li, Jing-Ran,Li, Dong-Dong,Wang, Rong-Rong,Sun, Jian,Dong, Jing-Jun,Du, Qian-Ru,Fang, Fei,Zhang, Wei-Ming,Zhu, Hai-Liang
, p. 438 - 447 (2014/03/21)
Components of fatty acid biosynthetic pathway have been identified as attractive targets for the development of new antibacterial agents. Compounds of series A (4a-4g) and series B (5a-5g) were synthesized by the formation of an amine bond between aromati
Design, synthesis and antibacterial activity studies of thiazole derivatives as potent ecKAS III inhibitors
Cheng, Kui,Xue, Jia-Yu,Zhu, Hai-Liang
, p. 4235 - 4238 (2013/07/26)
Two series of thiazole derivatives containing amide skeleton were synthesized and developed as potent Escherichia coli β-ketoacyl-(acyl- carrier-protein) synthase III (ecKAS III) inhibitors. All the 24 new synthesized compounds were assayed for antibacterial activity against the respective Gram-negative and Gram-positive bacterial strains, including E. coli, Pseudomonas aeruginosa, Bacillus subtilis and Staphylococcus aureus. In which, 10 compounds with broad-spectrum antibacterial activities were further tested for their ecKAS III inhibitory activity. Last, we have successfully found that compound 4e showed both the promising broad antibacterial activity with MIC of 1.56-6.25 μg/mL against the representative bacterial stains, and also processed the most potent ecKAS III inhibitory activity with IC50 of 5.3 μM. In addition, docking simulation also carried out in this study to give a potent prediction binding mode between the small molecule and ecKAS III (PDB code: 1hnj) protein.