1006-34-4Relevant 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.
Synthesis of 1-aminoisoquinolines by gold(III)-mediated domino reactions from 2-alkynylbenzamides and ammonium acetate
Long, Yuhua,She, Zhigang,Liu, Xiaochen,Chen, Yu
, p. 2579 - 2588 (2013/04/24)
A facile synthetic route toward pharmaceutically interesting 1-aminoisoquinoline derivatives by gold(III)-mediated domino reactions is described. This synthetic protocol starts from readily available 2-alkynylbenzamides and ammonium acetate and takes plac
2-[1-PHENYL-5-HYDROXY OR METHOXY-4ALPHA-METHYL-HEXAHYDROCLOPENTA[F]INDAZOL-5-YL]ETHYL PHENYL DERIVATIVES AS GLUCOCORTICOID RECEPTOR LIGANDS
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Page/Page column 59-60, (2008/12/05)
The present invention is directed to 2- [l-phenyl-5 -hydroxy or methoxy-4alpha- methyl-hexahydrocyclopenta[f]indazol-5-yl]ethyl phenyl derivatives of formula I (I) as glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflamma