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Miniaturized Modular Click Chemistry-enabled Rapid Discovery of Unique SARS-CoV-2 M Inhibitors With Robust Potency and Drug-like Profile.
Adv Sci (Weinh)
November 2024
Department of Medicinal Chemistry, Key Laboratory of Chemical Biology, Ministry of Education, School of Pharmaceutical Sciences, Shandong University, Ji'nan, 250012, China.
Article Synopsis
- * The novel compound C5N17B showed remarkable potency as an M inhibitor with low toxicity, performing better than existing medications like nirmatrelvir against multiple variants of SARS-CoV-2.
- * C5N17B also remains effective against resistant strains of the virus and has favorable pharmacokinetic properties, indicating its potential as a future treatment option for COVID-19.
CRISPR/Cas12a-drived electrochemiluminescence and fluorescence dual-mode magnetic biosensor for sensitive detection of Pseudomonas aeruginosa based on iridium(III) complex as luminophore.
Biosens Bioelectron
November 2024
School of Chemistry and Life Science, Jiangsu Key Laboratory for Environmental Functional Materials, Suzhou University of Science and Technology, Suzhou, Jiangsu, 215009, China. Electronic address:
The opportunistic human pathogen Pseudomonas aeruginosa (P. aeruginosa) poses a significant threat to human health, causing sepsis, inflammation, and pneumonia, so it is crucial to devise an expeditious detection platform for the P. aeruginosa.
View Article and Find Full Text PDFExpeditious Synthesis of Spiroindoline Derivatives via Tandem C(sp)-H and C(sp)-H Bond Functionalization of -Methyl--nitrosoanilines.
Org Lett
April 2024
State Key Laboratory of Antiviral Drugs, Pingyuan Laboratory, Key Laboratory of Green Chemical Media and Reactions, Ministry of Education, Collaborative Innovation Center of Henan Province for Green Manufacturing of Fine Chemicals, School of Chemistry and Chemical Engineering, Henan Normal University, Xinxiang, Henan 453007, China.
Presented herein is a novel synthesis of pharmaceutically privileged spiroindoline derivatives via cascade reactions of -methyl--nitrosoanilines with diazo homophthalimides. A group of mechanistic studies disclosed that the formation of product involves an unusual reaction mode of -methyl--nitrosoaniline featuring an initial C(sp)-H bond activation/alkylation followed by a C(sp)-H bond activation/spiroannulation. To our knowledge, this is the first example in which -methyl--nitrosoaniline acts as a C3N1 synthon to accomplish formal [4+1] spiroannulation with the participation of the -methyl unit rather than the previously reported C2N1 synthon to undergo formal [3+2] annulation without the participation of the -methyl unit.
View Article and Find Full Text PDFCompatibility of termination mechanisms in bacterial transcription with inference on eukaryotic models.
Biochem Soc Trans
April 2024
Department of Biological Sciences, and KAIST Stem Cell Center, Korea Advanced Institute of Science and Technology, Daejeon 34141, Republic of Korea.
Transcription termination has evolved to proceed through diverse mechanisms. For several classes of terminators, multiple models have been debatably proposed. Recent single-molecule studies on bacterial terminators have resolved several long-standing controversies.
View Article and Find Full Text PDFHerb-drug interactions of silybinin and cilofexor in beagle dogs based on pharmacokinetics by UPLC-MS/MS.
Front Pharmacol
February 2024
College of Basic Medicine and Forensic Medicine, Henan University of Science and Technology, Luoyang, Henan, China.
A remarkably sensitive, accurate, and efficient ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) approach was developed as a facile and expeditious method for measuring cilofexor concentration in beagle dogs, the herb-drug interactions between silybinin and cilofexor was explored based on pharmacokinetics. The plasma sample protein of the beagles were rapidly sedimented with acetonitrile, and cilofexor and tropifexor (internal standard, ISTD) were separated by gradient elution using a 0.1% formic acid aqueous solution and acetonitrile as the mobile phase.
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