cas 159803-11-9, 6-Fluoro-1,2-benzoisothiazol-3(2H)-one | Articles data ｜lookchem

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159803-11-9

Articles about 159803-11-9Total 3 be found

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Discovery of highly potent SARS-CoV-2 Mpro inhibitors based on benzoisothiazolone scaffold
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.
Chen, Weixiong,Feng, Bo,Han, Sheng,Wang, Peipei,Chen, Wuhong,Zang, Yi,Li, Jia,Hu, Youhong
(2022/01/14)

Concise approach to benzisothiazol-3(2 H)-one via copper-catalyzed tandem reaction of o -bromobenzamide and potassium thiocyanate in water
A concise approach to various benzisothiazol-3(2H)-one derivatives has been developed by copper-catalyzed the reaction of o-bromobenzamide derivatives with potassium thiocyanate (KSCN) in water. The reaction proceeds via a tandem reaction with S-C bond and S-N bond formation.
Wang, Fei,Chen, Chao,Deng, Geng,Xi, Chanjuan
experimental part
p. 4148 - 4151
(2012/06/18)

Antimicrobial activity of fluorinated 1,2-benzisothiazol-3(2H)-ones and 2,2'-dithiobis(benzamides)
Fluoro and trifluoromethyl derivatives of 1,2-benzisothiazol-3(2H)-ones and the 2,2'-dithiobis(benzamides) have been prepared and their antifungal and antibacterial activity evaluated. Several compounds were found highly active against fungi and Gram-positive microorganisms and a few derivatives displayed some activity against Gram-negative strains. Structure-activity relationships are proposed.
Carmellino,Pagani,Pregnolato,Terreni,Pastoni
p. 743 - 751
(2007/10/02)

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Chemical Properties

Density: 1.474 g/cm³
Storage Temp.:Sealed in dry,Room Temperature
Refractive Index: 1.63
PKA: 9.97±0.20(Predicted)
PSA: 61.10000
LogP: 1.72870

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