99848-43-8Relevant articles and documents
Discovery of highly potent SARS-CoV-2 Mpro inhibitors based on benzoisothiazolone scaffold
Chen, Weixiong,Feng, Bo,Han, Sheng,Wang, Peipei,Chen, Wuhong,Zang, Yi,Li, Jia,Hu, Youhong
supporting information, (2022/01/14)
The COVID-19 pandemic has drastically impacted global economies and public health. Although vaccine development has been successful, it was not sufficient against more infectious mutant strains including the Delta variant indicating a need for alternative treatment strategies such as small molecular compound development. In this work, a series of SARS-CoV-2 main protease (Mpro) inhibitors were designed and tested based on the active compound from high-throughput diverse compound library screens. The most efficacious compound (16b-3) displayed potent SARS-CoV-2 Mpro inhibition with an IC50 value of 116 nM and selectivity against SARS-CoV-2 Mpro when compared to PLpro and RdRp. This new class of compounds could be used as potential leads for further optimization in anti COVID-19 drug discovery.
Method for synthesizing chlorantraniliprole derivative intermediate
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, (2018/04/02)
The invention provides a method for synthesizing a chlorantraniliprole derivative intermediate, belonging to the field of agricultural pesticides. The method comprises the following steps: subjectingthe intermediate 3-bromo-1-(3-chloropyridin-2-yl)-1H-pyrazole-5-carboxylic acid to chlorination so as to prepare 3-bromo-1-(3-chloropyridin-2-yl)-1H-pyrazole-5-formyl chloride; subjecting the raw material 2-bromobenzoic acid to acylating chlorination and ammoniation so as to prepare substituted 2-bromo-benzamide; and subjecting 3-bromo-1-(3-chloropyridin-2-yl)-1H-pyrazole-5-formyl chloride and substituted 2-bromo-benzamide to cyclization so as to obtain the chlorantraniliprole derivative intermediate. The method of the invention is simple and common; reagents used in the process of synthesis are low in toxicity, used solvents are recyclable, and few by-products are produced, so the method has little corrosion to equipment and low pollution to environment; since raw materials are cheap, production cost is reduced and good economical efficiency is obtained; therefore, the method has good application prospects.
Certain pyrazoline derivatives with kinase inhibitory activity
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Page/Page column 105, (2008/12/06)
The present invention provides certain pyrazoline compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions and methods of using the compositions in the treatment of various diseases.