Frontiers | Hydrazones and Thiosemicarbazones Targeting Protein …
网页2022年4月10日 · Hydrazones and Thiosemicarbazones Targeting Protein-Protein-Interactions of SARS-CoV-2 Papain-like Protease. The papain-like protease (PLpro) of SARS-CoV-2 is essential for viral propagation and, additionally, dysregulation of the host innate immune system.
Hydrazones and Thiosemicarbazones Targeting Protein-Protein
网页2022年4月11日 · Here we describe the interaction of one hydrazone (H1) and five thiosemicarbazone (T1-T5) compounds with the two distinct natural substrate binding sites of PLpro for ubiquitin and ISG15. H1 binds to a polar groove at the S1 binding site by forming several hydrogen bonds with PLpro.
Mechanisms of SARS-CoV-2 entry into cells - Nature
网页2021年10月5日 · Introduction. Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is the causative agent of COVID-19, which escalated into a global pandemic in 2020. SARS-CoV-2 is an enveloped,...
Synthesis, characterization, DFT, antioxidant, antibacterial ...
网页2022年12月12日 · Three hydrazone derivatives have been synthesized using condensation reaction of 4-hydrazinylbenzoic acid with three aromatic aldehydes namely: thiophene-2-carbaldehyde, thiophene-3-carbaldehyde and 2-furaldehyde in ethanol at 78 °C reflux.
Synthesis, SARS-CoV-2 main protease inhibition ... - ScienceDirect
网页2024年4月1日 · Herein, a series of seven hybrid molecules (5a-5f, 5h) incorporating both furanochromene and quinoline moieties, linked by a hydrazone unit, was synthesized for evaluation of their SARS-CoV-2 M pro activity, using both experimental and molecular docking studies. The hydrazone unit was connected to the quinoline unit at different positions (2, 3 ...
Usnic acid based thiazole-hydrazones as multi-targeting …
网页2023年10月13日 · We synthesized a set of thiazolo-hydrazones based on (+)- and (−)-usnic acid and studied their ability to inhibit the main viral protease of the SARS-CoV-2 virus. It was shown that 9 out of 36 agents exhibit antiprotease activity in …
Synthesis, SARS-CoV-2 main protease inhibition, molecular
网页Seven furanochromene-quinoline derivatives containing a hydrazone linker were synthesized by condensing a furanochromene hydrazide with quinoline 2-, 3-, 4-, 5-, 6-, and 8-carbaldehydes, including 8-hydroxyquinoline-2-carbaldehye. Structure-activity correlations were investigated to determine the in ….
3. Molecular docking SARS-CoV-2 - National Center for …
网页2023年8月8日 · In the present work, we synthesize a new series of various tetrahydropyranone scaffolds containing hydrazones, oxime ether, triazole, and isoxazole to evaluate their antimicrobial, antitubercular, in silico SARS-CoV …
A SARS-CoV-2 protein interaction map reveals targets for drug …
网页2020年4月30日 · A human–SARS-CoV-2 protein interaction map highlights cellular processes that are hijacked by the virus and that can be targeted by existing drugs, including inhibitors of mRNA translation...
A Blueprint for High Affinity SARS-CoV-2 Mpro Inhibitors from …
网页2021年3月16日 · A potent SARS coronavirus (CoV) 3CL protease inhibitor (TG-0205221, Ki = 53 nM) has been developed. TG-0205221 showed remarkable activity against SARS CoV and human coronavirus (HCoV) 229E replications by reducing the viral titer by 4.7 log (at 5 μM) for SARS CoV and 5.2 log (at 1.25 μM) for HCoV 229E.
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