Published 2022
| Version v1
Journal article
Synthesis and SARS-CoV-2 3CL protease inhibitory effects of oxazolidinone derivatives
- 1. College of Science and Technology, Ningbo University, Cixi (China)
- 2. Xiamen University, South Xiang-An Road, Xiamen (China)
Description
The 3-chymotrypsin-like protease (3CLpro) is an attractive target for the development of anti-SARS (severe acute respiratory syndrome) drugs. In this work, a series of oxazolidinone derivatives 3a-3v were synthesized and their inhibitory activities against SARS coronavirus 2 (SARS-CoV-2) 3CLpro were evaluated by the fluorescence resonance energy transfer (FRET)-based enzymatic assay. Among synthesized compounds, 3g displayed the best inhibitory activity, with a half maximal inhibitory concentration (IC50) value of 14.47 μM. Also, docking studies implied that compound 3g was fitted into the active pocket of 3CLpro, forming a hydrogen bond with Glu166. (author)
Additional details
Publishing Information
- Journal Title
- Journal of the Brazilian Chemical Society (Online)
- Journal Volume
- 33
- Journal Issue
- 9
- Journal Page Range
- p. 1134-1143
- ISSN
- 1678-4790
INIS
- Country of Publication
- Brazil
- Country of Input or Organization
- Brazil
- INIS RN
- 53114647
- Subject category
- S37: INORGANIC, ORGANIC, PHYSICAL AND ANALYTICAL CHEMISTRY; S36: MATERIALS SCIENCE;
- Descriptors DEI
- CARBON 13; CHYMOTRYPSIN; CORONAVIRUSES; ENERGY TRANSFER; ENZYME INHIBITORS; HYDROGEN 1; NMR SPECTRA; OXAZOLES; RESONANCE FLUORESCENCE; SYNTHESIS
- Descriptors DEC
- AZOLES; CARBON ISOTOPES; DISEASES; EMISSION; ENZYMES; EVEN-ODD NUCLEI; FLUORESCENCE; HETEROCYCLIC COMPOUNDS; HYDROGEN ISOTOPES; HYDROLASES; INFECTIOUS DISEASES; ISOTOPES; LIGHT NUCLEI; LUMINESCENCE; MICROORGANISMS; NUCLEI; ODD-EVEN NUCLEI; ORGANIC COMPOUNDS; ORGANIC NITROGEN COMPOUNDS; ORGANIC OXYGEN COMPOUNDS; PARASITES; PEPTIDE HYDROLASES; PHOTON EMISSION; PROTEINS; SERINE PROTEINASES; SPECTRA; STABLE ISOTOPES; VIRAL DISEASES; VIRUSES; ZOONOTIC DISEASES