Abstract
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.
Highlights
Cancer is one of the main public health problems worldwide
The LLOQ was determined by analyzing the lowest concentration of the CNFD with relative standard deviation (RSD) and relative error (RE) lower than 20%
Stability results guaranteed the stability of CNFD in incubation conditions and auto-injector, since both the RE and RSD were lower than 8% (Table 1)
Summary
This study aimed to investigate the in vitro metabolism of this naphthoquinone by human liver microsomes. This study aimed to evaluate the in vitro metabolism of CNFD by CYP450 enzymes, including elucidation of the enzymatic kinetic profile, identification of the main CYP450 isoforms responsible for its metabolism, and prediction of in vivo pharmacokinetic parameters
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