A5013313442- HIV/AIDS drug development and treatment
- COVID-19 Clinical Research Studies
- SARS-CoV-2 and COVID-19 Research
- Viral gastroenteritis research and epidemiology
- Antibiotics Pharmacokinetics and Efficacy
- Biochemical and Molecular Research
- Cancer therapeutics and mechanisms
- Receptor Mechanisms and Signaling
- Traditional Chinese Medicine Analysis
- Phenothiazines and Benzothiazines Synthesis and Activities
- Respiratory viral infections research
- Chemical Synthesis and Reactions
- Analytical Chemistry and Chromatography
- Analytical Methods in Pharmaceuticals
- Chemical Synthesis and Analysis
- Pharmacological Receptor Mechanisms and Effects
- Carbohydrate Chemistry and Synthesis
- Neuroscience and Neuropharmacology Research
- Neurotransmitter Receptor Influence on Behavior
- Pneumocystis jirovecii pneumonia detection and treatment
- Inflammatory mediators and NSAID effects
- Boron Compounds in Chemistry
- Nanoplatforms for cancer theranostics
- Viral Infections and Immunology Research
- RNA Interference and Gene Delivery
Shanghai Institute of Materia Medica
2015-2022
Chinese Academy of Sciences
2015-2022
Henan Provincial People's Hospital
2020
Henan University
2020
University of Chinese Academy of Sciences
2018-2019
Shandong University
2014
Antibiotic (Bulgaria)
2013
Shandong Institute of Food and Drug Inspection
2012
Guangdong Institute for Drug Control
2011
State Institute for Drug Control
2007
The pandemic of coronavirus disease 2019 (COVID-19), caused by severe acute respiratory syndrome 2 (SARS-CoV-2), has become a global crisis. Replication SARS-CoV-2 requires the viral RNA-dependent RNA polymerase (RdRp) enzyme, target antiviral drug remdesivir. Here we report cryo-electron microscopy structure RdRp, both in apo form at 2.8-angstrom resolution and complex with 50-base template-primer remdesivir 2.5-angstrom resolution. reveals that partial double-stranded template is inserted...
VV116 (JT001) is an oral drug candidate of nucleoside analog against SARS-CoV-2. The purpose the three phase I studies was to evaluate safety, tolerability, and pharmacokinetics single multiple ascending doses in healthy subjects, as well effect food on safety VV116. Three were launched sequentially: Study 1 (single ascending-dose study, SAD), 2 (multiple MAD), 3 (food-effect FE). A total 86 subjects enrolled studies. tablets or placebo administered per protocol requirements. Blood samples...
The pandemic of Corona Virus Disease 2019 (COVID-19) caused by SARS-CoV-2 has become a global crisis. replication requires the viral RNA-dependent RNA polymerase (RdRp), direct target antiviral drug, Remdesivir. Here we report structure RdRp either in apo form or complex with 50-base template-primer and Remdesivir at resolution range 2.5-2.8 Å. reveals that partial double-stranded template is inserted into central channel where incorporated first replicated base pair terminates chain...
A novel synthetic route for making (−)-CBD and its derivatives bearing various C4′-side chains is developed by a late-stage diversification method. Starting from commercially available phloroglucinol, the key intermediate (−)-CBD-2OPiv-OTf efficiently regioselectively prepared further undergoes Negishi cross-coupling to furnish (−)-CBD. This approach allowed an efficient synthesis of in five-step total 52% yield on 10 g scale. Furthermore, chain with this method can be realized wide range.
Currently, remdesivir is the first and only FDA-approved antiviral drug for COVID-19 treatment. Adequate supplies of are highly warranted to cope with this global public health crisis. Herein, we report a Weinreb amide approach preparing key intermediate in glycosylation step where overaddition side reactions eliminated. Starting from 2,3,5-tri-O-benzyl-d-ribonolactone, preferred route consisting three sequential steps (Weinreb amidation, O-TMS protection, Grignard addition) enables...
A one-pot process for preparing molnupiravir from cytidine was developed. The advantages of this synthesis were as follows: (1) presence N,N-dimethylformamide dimethyl acetal (DMF-DMA) facilitated the selective protection 2′,3′-dihydroxyls and amino cytidine, which eliminated negative impact these groups on following isobutyrylation at 5′-hydroxyl. (2) Degradations product in deprotection stage avoided since a mild condition used. (3) achievement hydroxyamination one single step improved...
SARS-CoV-2 has caused a global pandemic of COVID-19 that urgently needs an effective treatment. Nucleoside analog drugs including favipiravir have been repurposed for despite unclear mechanism their inhibition the viral RNA polymerase (RdRp). Here we report cryo-EM structures RdRp in complex with and two other nucleoside inhibitor ribavirin penciclovir. Ribavirin ribosylated form share similar ribose scaffold is distinct from However, reveal all three inhibitors are covalently linked to...
Alkylboronate derivatives are important intermediates in organic synthesis and medicinal chemistry. The research of synthesizing alkylboronic acid has attracted great attention chemists many papers have reported various methods for preparing alkylboronates based on transition-metal-catalyzed hydroboration. In this review, we summarize the alkylboronate with different catalysts, such as Rhodium, Palladium, Copper, Iridium, Iron, Magnesiu, Platinum, Nickel so on. Pinacolborane,...
Colorectal cancer (CRC) ranks as the third most prevalent global malignancy, marked by significant metastasis and post-surgical recurrence, posing formidable challenges to treatment efficacy. The integration of oligonucleotides with chemotherapeutic drugs emerges a promising strategy for synergistic CRC therapy. nanoformulation, lipid nanoparticle (LNP), presents capability achieve co-delivery In this study, we constructed nanoparticles, termed LNP-I-V microfluidics co-deliver miR159 mimics...
We reported the synthesis and anti-RSV or anti-IFV activities of NHC derivatives 4′-fluorouridine prodrugs, which were evaluated for their chemical stability PK properties. Tri-isobutyrate ester 1a has potential to be as an antiviral agent.
A novel and efficient method for the aminolysis of trizole epoxides is described. This consists a facile ring opening mediated by t-BuOMgCl generated in situ from amine hydrochlorides (t-BuO)2Mg. The desired β-amino alcohols were obtained good yields without employing other heavy metals or precious catalysts. optimized conditions successfully applied to synthesis number potential triazole antifungal compounds as well efinaconazole on up 700 g scale.