1736-72-7Relevant articles and documents
Discovery of aminothiazole derivatives as novel human enterovirus A71 capsid protein inhibitors
Cai, Yang,Chen, Yinuo,Dong, Chune,Lan, Ke,Lei, Ping,Tang, Qi,Wu, Shuwen,Xu, Ting,Xu, Zhichao,Zhou, Hai-Bing,Zou, Wenting
, (2022/03/15)
Enterovirus A71 (EV-A71), one of the major pathogens that causes hand, foot and mouth disease (HFMD), has seriously threatened the health and safety of young children. In this study, aminothiazole derivatives were synthesized and screened against EV-A71 in Rhabdomyosarcoma (RD) cells. The best compound (12s), with a biphenyl group, showed activity against EV-A71 (EC50: 0.27 μM) but also against a series of different human enteroviruses without significant cytotoxicity (CC50 > 56.2 μM). Mechanistic studies including time-of-drug-addition assays, viral entry assays and microscale thermophoresis (MST) experiments, showed that 12s binds to EV-A71 capsid and blocks the binding between the viral protein VP1 and the relevant human scavenger receptor class B member 2 (hSCARB2).
Novel arylimino thiazole compound, preparation method and uses thereof
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Paragraph 0125; 0126; 0127; 0128, (2018/03/28)
The present invention relates to a compound with antibacterial synergy activity, a preparation and uses thereof, particularly to a novel arylimino thiazole compound, a preparation method and uses thereof, and specifically discloses a class of compounds represented by a formula (I) or optical isomers, cis-trans isomers or pharmaceutically acceptable salts thereof, a preparation method and uses thereof. The invention further discloses a pharmaceutical composition containing the compound. The compound of the present invention can effectively enhance the antibacterial activity of antibiotics, andcan be used for treating antibiotic-resistant bacteria. The formula (I) is defined in the specification.
2-(4-trifluoromethyl-phenylimino)-5-(2-naphthyl)methylene-thiazolidin-4-one compound and application thereof
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Paragraph 0022; 0023; 0028, (2017/07/22)
The invention discloses a thiazole heterocyclic compound. The thiazole heterocyclic compound is 2-(4-trifluoromethyl-phenylimino)-5-(2-naphthyl) methylene-thiazolidin-4-one compound, which is referred as TNTO and has a chemical structure as shown in a general formula (I). The invention further discloses an application of the compound as an aromatic hydrocarbon receptor stimulant. Experiments prove that the thiazole heterocyclic compound under the concentration of 10 muM can remarkably up-regulate the gene, protein expression of the related exogenous substance metabolic enzyme CYP1A1 of the downstream target gene of the aromatic hydrocarbon receptor in the mouse liver cancer cells, the compound is prompted to be an agonist of an aromatic hydrocarbon receptor, and is expected to become a potential medicine which takes the aromatic hydrocarbon receptor as the tumor target, and has wide clinical application prospect and economic development value.