25100-91-8Relevant academic research and scientific papers
Relative hepatotoxicity of 2-(substituted phenyl)thiazoles and substituted thiobenzamides in mice: Evidence for the involvement of thiobenzamides as ring cleavage metabolites in the hepatotoxicity of 2-phenylthiazoles
Mizutani,Suzuki
, p. 101 - 105 (1996)
The hepatotoxicity of the 3 isomers of para-substituted thiobenzamides and the 3 isomers of 2-(para-substituted phenyl)-4-methylthiazoles was evaluated in mice depleted of glutathione (GSH) by pretreatment with buthionine sulfoximine (BSO). In accordance
PdII-Catalyzed Regio- and Enantioselective Oxidative C?H/C?H Cross-Coupling Reaction between Ferrocenes and Azoles
Cai, Zhong-Jian,Liu, Chen-Xu,Gu, Qing,Zheng, Chao,You, Shu-Li
supporting information, p. 2149 - 2153 (2019/01/24)
Asymmetric C?H bond functionalization reaction is one of the most efficient and straightforward methods for the synthesis of optically active molecules. Herein we disclose an asymmetric C?H/C?H cross-coupling reaction of ferrocenes with azoles such as oxazoles and thiazoles. Palladium(II)/monoprotected amino acid (MPAA) catalytic system which exhibits excellent reactivity and regioselectivity for oxazoles and thiazoles. This method offers a powerful strategy for constructing planar chiral ferrocenes. Mechanistic studies suggest that the C?H bond cleavage of azoles is likely proceeding through a SEAr process and may not be a turnover limiting step.
Pd/Cu-cocatalyzed reigoselective arylation of thiazole derivatives at 2-position under ligand-free conditions
Gu, Jian,Cai, Chun
, p. 56311 - 56315 (2015/07/15)
An efficient protocol for regioselective arylation of thiazole derivatives at the 2-position via palladium- and copper-catalyzed C-H bond activation under ligand-free conditions has been developed. The reaction proceeds smoothly with 1% palladium catalyst in the presence of 20% Cu(TFA)2 to furnish the desired products. The direct C-H arylation and no ligand made this method synthetically useful for the arylation of thiazoles at the 2-position.
Design, synthesis, and biological evaluation of antiviral agents targeting flavivirus envelope proteins
Li, Ze,Khaliq, Mansoora,Zhou, Zhigang,Post, Carol Beth,Kuhn, Richard J.,Cushman, Mark
experimental part, p. 4660 - 4671 (2009/07/11)
Flavivirus envelope proteins (E proteins) have been shown to play a pivotal role in virus assembly, morphogenesis, and infection of host cells. Inhibition of flavivirus infection of a host cell by means of a small molecule envelope protein antagonist is an attractive strategy for the development of antiviral agents. Virtual screening of the NCI chemical database using the dengue virus envelope protein structure revealed several hypothetical hit compounds. Bioassay results identified a class of thiazole compounds with antiviral potency in cell-based assays. Modification of these lead compounds led to a series of analogues with improved antiviral activity and decreased cytotoxicity. The most active compounds 11 and 36 were effective in the low micromolar concentration range in a cellular assay system.
