328268-69-5Relevant academic research and scientific papers
Substituted thiazole ketones secreted aspartic protease inhibitors and its preparation method
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Paragraph 0107, (2017/08/31)
The invention relates to a substituted thiazole ketones secretory aspartic protease inhibitor and a preparation method thereof, and particularly provides a novel thiazole ketones compound. The general structural formula of the novel thiazole ketones compound is shown as follows. The thiazole ketones compound is high in Sap2 enzyme inhibiting activity and nematode and mouse in-vivo antifungal activity, and has good antifungal medicine combination effect on fluconazole resistant bacteria, thereby being capable of being used for preparing medicine for preventing fungal infection or being combined with existing antifungal medicine. A new approach is created for deeply studying and developing novel antifungal medicine.
Synthesis of novel 4-thiazolidione derivatives as antibacterial agents against drug-resistant Staphylococcus epidermidis
Zhao, Dan,Liu, Huayong,Zheng, Likang,He, Guozhen,Qu, Di,Han, Shiqing
, p. 3743 - 3750 (2013/07/26)
A series of novel substituted 4-thiazolidione derivatives were designed, synthesized, and evaluated in vitro for their antibacterial activities, in comparison with methicillin and ampicillin. Compounds (7d, 7h-k) exhibit good potency in inhibiting the growth of Staphylococcus epidermidis (MIC: 1.57-3.13 μM). Further antibacterial effects of compounds (7d, 7h-k) were investigated using clinical isolates (methicillin-resistant Staphylococcus epidermidis and methicillin-resistant Staphylococcus aureus), in comparison with methicillin and levofloxacin. Compound 7k showed the most potent antibacterial activities among the synthesized compounds.
