1344678-60-9Relevant academic research and scientific papers
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.
A Benz thiazolinone acetyl amine derivative and its synthetic method and application
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Paragraph 0020-0022, (2017/11/24)
The invention discloses benzisothiazolone acetamide derivatives and a synthetic method and an application thereof, and the series of compounds are compounds represented by the general formula (I), wherein R is hydrogen, 2-methoxy, 4-methoxy, 4-bromo, 2,6-
Antifungal activity of a series of 1,2-benzisothiazol-3(2H)-one derivatives
Dou, Dengfeng,Alex, Deepu,Du, Bingfan,Tiew, Kok-Chuan,Aravapalli, Sridhar,Mandadapu, Sivakoteswara Rao,Calderone, Richard,Groutas, William C.
experimental part, p. 5782 - 5787 (2011/10/19)
A series of broad-spectrum antifungal agents based on the 1,2-benzisothiazol-3(2H)-one scaffold is reported. Preliminary structure-activity relationship studies have established the importance of the presence of the heterocyclic ring, a methyl group, and
