16777-78-9Relevant articles and documents
Discovery of Novel Thiophene-arylamide Derivatives as DprE1 Inhibitors with Potent Antimycobacterial Activities
Wang, Pengxu,Batt, Sarah M.,Wang, Bin,Fu, Lei,Qin, Rongfei,Lu, Yu,Li, Gang,Besra, Gurdyal S.,Huang, Haihong
, p. 6241 - 6261 (2021/05/06)
In this study, we report the design and synthesis of a series of novel thiophene-arylamide compounds derived from the noncovalent decaprenylphosphoryl-β-d-ribose 2′-epimerase (DprE1) inhibitor TCA1 through a structure-based scaffold hopping strategy. Systematic optimization of the two side chains flanking the thiophene core led to new lead compounds bearing a thiophene-arylamide scaffold with potent antimycobacterial activity and low cytotoxicity. Compounds 23j, 24f, 25a, and 25b exhibited potent in vitro activity against both drug-susceptible (minimum inhibitory concentration (MIC) = 0.02-0.12 μg/mL) and drug-resistant (MIC = 0.031-0.24 μg/mL) tuberculosis strains while retaining potent DprE1 inhibition (half maximal inhibitory concentration (IC50) = 0.2-0.9 μg/mL) and good intracellular antimycobacterial activity. In addition, these compounds showed good hepatocyte stability and low inhibition of the human ether-à-go-go related gene (hERG) channel. The representative compound 25a with acceptable pharmacokinetic property demonstrated significant bactericidal activity in an acute mouse model of tuberculosis. Moreover, the molecular docking study of template compound 23j provides new insight into the discovery of novel antitubercular agents targeting DprE1.
A nanowire the platinum accepts method for catalytic synthesis of amides (by machine translation)
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Paragraph 0071-0073, (2017/02/28)
The invention relates to a nanowire the platinum accepts method for catalytic synthesis of amides. Specifically, the method comprises the following steps: adding the reaction vessel in the nanowire the platinum accepts in alcoholic, decompression except mellow, further adding alchlor, reaction solvent, pyridine, amine compounds, aldehyde compound and an oxidizing agent, under the mixing conditions, the heating reaction in in oil bath, after purification by column chromatography, to obtain amides, wherein: the states the aldehyde class compounds, amine compounds, alchlor, pyridine, the platinum accepts molar ratio of the oxidizing agent and 0.5-3 : 0.5-3 : 0.1-0.5: 0.5-2 : 0.1% - 2% : 0.5-5, the heating of the reaction temperature is 80-140°C, the reaction time is 16-24 hours. Because the nanowire the platinum accepts as the catalyst, the invention is not only high catalytic activity, and the performance is stable, at the same time the method of the present invention can obtain a higher yield, mild condition, process is simple, easy to operate. (by machine translation)
Thermoplastic polymer composition
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, (2015/12/17)
The invention provides a compound conforming to the structure of Formula (C) The invention also provides a thermoplastic polymer composition comprising a polyolefin polymer and a compound conforming to the structure of Formula (C) as a nucleating agent.