42,382 results match your criteria Antiviral chemistry & chemotherapy[Journal]


Novel therapeutic approaches for treatment of COVID-19.

J Mol Med (Berl) 2020 Jun 3. Epub 2020 Jun 3.

Department of Regenerative Medicine, Cell Science Research Center, Royan Institute for Stem Cell Biology and Technology, ACECR, Tehran, Iran.

To date, there is no licensed treatment or approved vaccine to combat the coronavirus disease of 2019 (COVID-19), and the number of new cases and mortality multiplies every day. Therefore, it is essential to develop an effective treatment strategy to control the virus spread and prevent the disease. Here, we summarized the therapeutic approaches that are used to treat this infection. Read More

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http://dx.doi.org/10.1007/s00109-020-01927-6DOI Listing

Linking indirect effects of cytomegalovirus in transplantation to modulation of monocyte innate immune function.

Sci Adv 2020 Apr 22;6(17):eaax9856. Epub 2020 Apr 22.

Center for Immunology and Inflammatory Diseases, Massachusetts General Hospital and Harvard Medical School, Boston, MA, USA.

Cytomegalovirus (CMV) is an important cause of morbidity and mortality in the immunocompromised host. In transplant recipients, a variety of clinically important "indirect effects" are attributed to immune modulation by CMV, including increased mortality from fungal disease, allograft dysfunction and rejection in solid organ transplantation, and graft-versus-host-disease in stem cell transplantation. Monocytes, key cellular targets of CMV, are permissive to primary, latent and reactivated CMV infection. Read More

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http://dx.doi.org/10.1126/sciadv.aax9856DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7176434PMC

Multi-sulfonated ligands on gold nanoparticles as virucidal antiviral for Dengue virus.

Sci Rep 2020 Jun 3;10(1):9052. Epub 2020 Jun 3.

Laboratory for personalized medicine, IRCCS Ospedale Specializzato in Gastroenterologia "Saverio de Bellis", Castellana Grotte, BA, Italy.

Dengue virus (DENV) causes 390 million infections per year. Infections can be asymptomatic or range from mild fever to severe haemorrhagic fever and shock syndrome. Currently, no effective antivirals or safe universal vaccine is available. Read More

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http://dx.doi.org/10.1038/s41598-020-65892-3DOI Listing

Investigation of Some Antiviral -Heterocycles as COVID 19 Drug: Molecular Docking and DFT Calculations.

Int J Mol Sci 2020 May 30;21(11). Epub 2020 May 30.

Chemistry Department, College of Sciences, Al-Madina Al-Munawarah, Taibah University, Al-Madina 30002, Saudi Arabia.

The novel coronavirus, COVID-19, caused by SARS-CoV-2, is a global health pandemic that started in December 2019. The effective drug target among coronaviruses is the main protease M, because of its essential role in processing the polyproteins that are translated from the viral RNA. In this study, the bioactivity of some selected heterocyclic drugs named Favipiravir (), Amodiaquine (), 2'-Fluoro-2'-deoxycytidine (), and Ribavirin () was evaluated as inhibitors and nucleotide analogues for COVID-19 using computational modeling strategies. Read More

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http://dx.doi.org/10.3390/ijms21113922DOI Listing

(Iso)Quinoline-Artemisinin Hybrids via Click Chemistry: Highly Potent Agents against Viruses.

Chemistry 2020 Jun 2. Epub 2020 Jun 2.

Institut für Organische Chemie, Friedrich-Alexander Universität Erlangen-Nürnberg, Department Chemie und Pharmazie, Henkestrasse 42, 91054, Erlangen, GERMANY.

Viral infections cause life-threatening diseases in millions of people worldwide every year and there is urgent need for new effective antiviral drugs. Hybridization of two chemically diverse compounds into a new bioactive effector product is a successful concept to improve the hybrid drug's properties compared to its parent compounds. In this study, (iso)quinoline-artemisinin hybrids, obtained via copper-catalyzed azide-alkyne cycloaddition (CuAAC) or organocatalyzed click reactions (in organic solvents or in the presence of water), were analyzed in vitro for the first time for their inhibitory activity against human cytomegalovirus (HCMV), as compared with their parent compounds and the reference drug ganciclovir. Read More

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http://dx.doi.org/10.1002/chem.202001803DOI Listing

Medicinal chemistry strategies of targeting HIV-1 capsid protein for antiviral treatment.

Future Med Chem 2020 Jun 2. Epub 2020 Jun 2.

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012 Jinan, Shandong, PR China.

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http://dx.doi.org/10.4155/fmc-2020-0084DOI Listing

Visualizing Tetrahedral Oxyanion Bound in HIV-1 Protease Using Neutrons: Implications for the Catalytic Mechanism and Drug Design.

ACS Omega 2020 May 14;5(20):11605-11617. Epub 2020 May 14.

Neutron Scattering Division, Oak Ridge National Laboratory, Oak Ridge, Tennessee 37830, United States.

HIV-1 protease is indispensable for virus propagation and an important therapeutic target for antiviral inhibitors to treat AIDS. As such inhibitors are transition-state mimics, a detailed understanding of the enzyme mechanism is crucial for the development of better anti-HIV drugs. Here, we used room-temperature joint X-ray/neutron crystallography to directly visualize hydrogen atoms and map hydrogen bonding interactions in a protease complex with peptidomimetic inhibitor KVS-1 containing a reactive nonhydrolyzable ketomethylene isostere, which, upon reacting with the catalytic water molecule, is converted into a tetrahedral intermediate state, KVS-1. Read More

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http://dx.doi.org/10.1021/acsomega.0c00835DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7254801PMC

Ethnobotany and Antimicrobial Peptides From Plants of the Solanaceae Family: An Update and Future Prospects.

Front Pharmacol 2020 7;11:565. Epub 2020 May 7.

Pharmacy Discipline, Life Science School, Khulna University, Khulna, Bangladesh.

The Solanaceae is an important plant family that has been playing an essential role in traditional medicine and human nutrition. Members of the Solanaceae are rich in bioactive metabolites and have been used by different tribes around the world for ages. Antimicrobial peptides (AMPs) from plants have drawn great interest in recent years and raised new hope for developing new antimicrobial agents for meeting the challenges of antibiotic resistance. Read More

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http://dx.doi.org/10.3389/fphar.2020.00565DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7232569PMC

Virtual Screening-Driven Drug Discovery of SARS-CoV2 Enzyme Inhibitors Targeting Viral Attachment, Replication, Post-Translational Modification and Host Immunity Evasion Infection Mechanisms.

J Biomol Struct Dyn 2020 Jun 1:1-23. Epub 2020 Jun 1.

Laboratory for Organic Reactivity, Discovery and Synthesis (LORDS), Research Center for the Natural and Applied Sciences, University of Santo Tomas, España Blvd., Manila 1015, Philippines.

The novel coronavirus SARS-CoV2, the causative agent of the pandemic disease COVID-19, emerged in December 2019 forcing lockdown of communities in many countries. The absence of specific drugs and vaccines, the rapid transmission of the virus, and the increasing number of deaths worldwide necessitated the discovery of new substances for anti-COVID-19 drug development. With the aid of bioinformatics and computational modelling, ninety seven antiviral secondary metabolites from fungi were docked onto five SARS-CoV2 enzymes involved in viral attachment, replication, post-translational modification, and host immunity evasion infection mechanisms followed by molecular dynamics simulation and ADMET prediction (absorption, distribution, metabolism, excretion and toxicity) of the hit compounds. Read More

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http://dx.doi.org/10.1080/07391102.2020.1776639DOI Listing

Pharmacological Agents Targeting Thromboinflammation in COVID-19: Review and Implications for Future Research.

Thromb Haemost 2020 May 30. Epub 2020 May 30.

Liverpool Centre for Cardiovascular Science, University of Liverpool and Liverpool Heart and Chest Hospital, Liverpool, United Kingdom.

Coronavirus disease 2019 (COVID-19), currently a worldwide pandemic, is a viral illness caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). The suspected contribution of thrombotic events to morbidity and mortality in COVID-19 patients has prompted a search for novel potential options for preventing COVID-19-associated thrombotic disease. In this article by the Global COVID-19 Thrombosis Collaborative Group, we describe novel dosing approaches for commonly used antithrombotic agents (especially heparin-based regimens) and the potential use of less widely used antithrombotic drugs in the absence of confirmed thrombosis. Read More

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http://dx.doi.org/10.1055/s-0040-1713152DOI Listing

Prediction of Novel Inhibitors of the Main Protease (M-pro) of SARS-CoV-2 through Consensus Docking and Drug Reposition.

Int J Mol Sci 2020 May 27;21(11). Epub 2020 May 27.

Departament de Bioquímica i Biotecnologia, Research group in Cheminformatics & Nutrition, Campus de Sescelades, Universitat Rovira i Virgili, 43007 Tarragona, Catalonia, Spain.

Since the outbreak of the COVID-19 pandemic in December 2019 and its rapid spread worldwide, the scientific community has been under pressure to react and make progress in the development of an effective treatment against the virus responsible for the disease. Here, we implement an original virtual screening (VS) protocol for repositioning approved drugs in order to predict which of them could inhibit the main protease of the virus (M-pro), a key target for antiviral drugs given its essential role in the virus' replication. Two different libraries of approved drugs were docked against the structure of M-pro using Glide, FRED and AutoDock Vina, and only the equivalent high affinity binding modes predicted simultaneously by the three docking programs were considered to correspond to bioactive poses. Read More

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http://dx.doi.org/10.3390/ijms21113793DOI Listing

Excess Ascorbate is a Chemical Stress Agent against Proteins and Cells.

Pharmaceuticals (Basel) 2020 May 27;13(6). Epub 2020 May 27.

Department of Chemistry, Babes-Bolyai University, 400028 Cluj-Napoca, Romania.

Excess ascorbate (as expected in intravenous treatment proposed for COVID-19 management, for example) oxidizes and/or degrades hemoglobin and albumin, as evidenced by UV-vis spectroscopy, gel electrophoresis, and mass spectrometry. It also degrades hemoglobin in intact blood or in isolated erythrocytes. The survival rates and metabolic activities of several leukocyte subsets implicated in the antiviral cellular immune response are also affected. Read More

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http://dx.doi.org/10.3390/ph13060107DOI Listing

C-H functionalization of quinazolinones by transition metal catalysis.

Org Biomol Chem 2020 May 29. Epub 2020 May 29.

Department of Chemistry, University of North Bengal, Darjeeling - 734013, India.

Quinazolinone and its congeners are ubiquitous structural motifs found in numerous natural products due to their wide applications as anticancer, antiviral, anti-inflammatory, antifolate and antitumor agents etc. Previously, the synthetic community devoted their efforts towards synthetic approaches but recent years have also witnessed an upsurge in the diversification of this scaffold and its applications. Thus, this review (from 2011 to the beginning of 2020) comprehensively focuses on transition metal catalyzed C-H bond functionalization namely arylation, amination, acetoxylation, amidation, alkylation, alkenylation, alkynylation, halogenation, thiolation, trifluoroethylation etc. Read More

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http://dx.doi.org/10.1039/d0ob00742kDOI Listing

Docking study of Chloroquine and Hydroxychloroquine interaction with SARS-CoV-2 spike glycoprotein-An insight into the comparative efficacy of repurposing antiviral drugs.

J Biomol Struct Dyn 2020 May 29:1-11. Epub 2020 May 29.

Department of Chemistry, University of Sargodha, Sargodha-40100, Pakistan.

Recent outbreak of novel Coronavirus disease (Covid-19) pandemic around the world is associated with severe acute respiratory syndrome. The death toll associated with the pandemic is increasing day by day. SARS-CoV-2 is an enveloped virus and there are ample evidences that its Spike protein (S-protein) is mainly associated with pathogenesis as it is surface-exposed and mediates entry into host cells by binding to angiotensin-converting enzyme-2 (ACE-2) receptor. Read More

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http://dx.doi.org/10.1080/07391102.2020.1775703DOI Listing

Inhibitory antibodies identify unique sites of therapeutic vulnerability in rhinovirus and other enteroviruses.

Proc Natl Acad Sci U S A 2020 May 28. Epub 2020 May 28.

Shanghai Institute for Advanced Immunochemical Studies, ShanghaiTech University, 201210 Shanghai, People's Republic of China;

The existence of multiple serotypes renders vaccine development challenging for most viruses in the genus. An alternative and potentially more viable strategy for control of these viruses is to develop broad-spectrum antivirals by targeting highly conserved proteins that are indispensable for the virus life cycle, such as the 3C protease. Previously, two single-chain antibody fragments, YDF and GGVV, were reported to effectively inhibit human rhinovirus 14 proliferation. Read More

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http://dx.doi.org/10.1073/pnas.1918844117DOI Listing

Experimental Data Based Machine Learning Classification Models with Predictive Ability to Select in Vitro Active Antiviral and Non-Toxic Essential Oils.

Molecules 2020 May 25;25(10). Epub 2020 May 25.

Rome Center for Molecular Design, Department of Drug Chemistry and Technology, Sapienza University, P.le Aldo Moro 5, 00185 Rome, Italy.

In the last decade essential oils have attracted scientists with a constant increase rate of more than 7% as witnessed by almost 5000 articles. Among the prominent studies essential oils are investigated as antibacterial agents alone or in combination with known drugs. Minor studies involved essential oil inspection as potential anticancer and antiviral natural remedies. Read More

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http://dx.doi.org/10.3390/molecules25102452DOI Listing

In Vitro and In Vivo Antiviral Activity of Nylidrin by Targeting the Hemagglutinin 2-Mediated Membrane Fusion of Influenza A Virus.

Viruses 2020 May 25;12(5). Epub 2020 May 25.

Infectious Diseases Therapeutic Research Center, Korea Research Institute of Chemical Technology (KRICT), Daejeon 34114, Korea.

Influenza A virus, one of the major human respiratory pathogens, is responsible for annual seasonal endemics and unpredictable periodic pandemics. Despite the clinical availability of vaccines and antivirals, the antigenic diversity and drug resistance of this virus makes it a persistent threat to public health, underlying the need for the development of novel antivirals. In a cell culture-based high-throughput screen, a β2-adrenergic receptor agonist, nylidrin, was identified as an antiviral compound against influenza A virus. Read More

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http://dx.doi.org/10.3390/v12050581DOI Listing

Porcine epidemic diarrhea virus deficient in RNA cap guanine-N-7 methylation is attenuated and induces higher type I and III interferon responses.

J Virol 2020 May 27. Epub 2020 May 27.

College of Veterinary Medicine, Nanjing Agricultural University, Nanjing, Jiangsu, P. R. China 210095

The 5' cap methylation of viral RNA plays an important role in RNA stability, efficient translation, and immune evasion. Thus, RNA cap methylation is an attractive target for antiviral discovery and development of new live attenuated vaccines. For coronaviruses, RNA cap structure is first methylated at guanine N-7 (G-N-7) position by nonstructural protein 14 (nsp14), which facilitates and precedes the subsequent ribose 2'-O methylation by nsp16-nsp10 complex. Read More

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http://dx.doi.org/10.1128/JVI.00447-20DOI Listing

Remdesivir for Treatment of COVID-19: Combination of Pulmonary and IV Administration May Offer Aditional Benefit.

Authors:
Duxin Sun

AAPS J 2020 05 26;22(4):77. Epub 2020 May 26.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Michigan, Ann Arbor, Michigan, 48109, USA.

Remdesivir is one of the most promising drugs to treat COVID-19 based on the following facts: remdesivir has a broad-spectrum antiviral mechanism of action; it demonstrated in vitro activity against SARS-CoV-2 and in vivo efficacy in animal models against the similar coronavirus MERS-CoV; its safety profile has been tested in Ebola patients and in compassionate use in COVID-19 patients. Currently, remdesivir is being investigated in ten randomized controlled trials against COVID-19. The dose regimen of remdesivir is an IV loading dose of 200 mg on day 1 followed by daily IV maintenance doses of 100 mg for 5-9 days. Read More

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http://dx.doi.org/10.1208/s12248-020-00459-8DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7250281PMC

Potential Inhibitors for Novel Coronavirus Protease Identified by Virtual Screening of 606 Million Compounds.

Int J Mol Sci 2020 May 21;21(10). Epub 2020 May 21.

Computational Pharmacy, Department of Pharmaceutical Sciences, University of Basel, 4056 Basel, Switzerland.

The rapid outbreak of the novel severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in China followed by its spread around the world poses a serious global concern for public health. To this date, no specific drugs or vaccines are available to treat SARS-CoV-2 despite its close relation to the SARS-CoV virus that caused a similar epidemic in 2003. Thus, there remains an urgent need for the identification and development of specific antiviral therapeutics against SARS-CoV-2. Read More

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http://dx.doi.org/10.3390/ijms21103626DOI Listing

Theoretical Study on Ionization of Boric Acid in Aqueous Solution by and DFT Methods at T=298.15 K.

Turk J Pharm Sci 2020 Apr 24;17(2):177-181. Epub 2020 Apr 24.

Department of Chemistry, Faculty of Science, Ayatollah Amoli Branch, Islamic Azad University, Amol, Iran.

Objectives: The aim of this research work was to theoretically calculate the pK value of boric acid in aqueous solution by theoretical methods at T=298.15 K.

Materials And Methods: Boric acid has antifungal and antiviral properties. Read More

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http://dx.doi.org/10.4274/tjps.galenos.2018.26818DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7227919PMC

Post-Translation Regulation of Influenza Virus Replication.

Annu Rev Virol 2020 May 26. Epub 2020 May 26.

Department of Medical Microbiology and Immunology, University of Wisconsin-Madison, Madison, Wisconsin 53706, USA; email:

Influenza virus exploits cellular factors to complete each step of viral replication. Yet, multiple host proteins actively block replication. Consequently, infection success depends on the relative speed and efficacy at which both the virus and host use their respective effectors. Read More

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http://dx.doi.org/10.1146/annurev-virology-010320-070410DOI Listing

An RNA-dependent RNA polymerase inhibitor for tick-borne encephalitis virus.

Virology 2020 Jul 25;546:13-19. Epub 2020 Mar 25.

Department of Biological and Agricultural Engineering, Texas A&M University, College Station, United States. Electronic address:

Tick-borne encephalitis virus (TBEV) is a medically important representative of the Flaviviridae family. The TBEV genome encodes a single polyprotein, which is co/post-translationally cleaved into three structural and seven non-structural proteins. Of the non-structural proteins, NS5, contains an RNA-dependent RNA polymerase (RdRp) domain that is highly conserved and is responsible for the genome replication. Read More

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http://dx.doi.org/10.1016/j.virol.2020.03.006DOI Listing

Protease Inhibitors: Candidate Drugs to Inhibit Severe Acute Respiratory Syndrome Coronavirus 2 Replication.

Tohoku J Exp Med 2020 05;251(1):27-30

Laboratory of Health and Sports Science, Division of Biomedical Engineering for Health and Welfare, Tohoku University Graduate School of Biomedical Engineering.

The number of patients infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has rapidly increased, although the WHO declared a pandemic. However, drugs that function against SARS-CoV-2 have not been established. SARS-CoV-2 has been suggested to bind angiotensin-converting enzyme 2, the receptor of the SARS coronavirus. Read More

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http://dx.doi.org/10.1620/tjem.251.27DOI Listing

Evaluation of the efficacy and safety of intravenous remdesivir in adult patients with severe COVID-19: study protocol for a phase 3 randomized, double-blind, placebo-controlled, multicentre trial.

Trials 2020 May 24;21(1):422. Epub 2020 May 24.

Department of Pulmonary and Critical Care Medicine, Center of Respiratory Medicine, National Clinical Research Center for Respiratory Diseases, China-Japan Friendship Hospital, Beijing, China.

Background: Coronavirus disease 2019 (COVID-19), caused by a novel corinavirus (later named SARS-CoV-2 virus), was fistly reported in Wuhan, Hubei Province, China towards the end of 2019. Large-scale spread within China and internationally led the World Health Organization to declare a Public Health Emergency of International Concern on 30 January 2020. The clinical manifestations of COVID-19 virus infection include asymptomatic infection, mild upper respiratory symptoms, severe viral pneumonia with respiratory failure, and even death. Read More

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http://dx.doi.org/10.1186/s13063-020-04352-9DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7245636PMC
May 2020
2.117 Impact Factor

A Review on the Progress and Prospects of Dengue Drug Discovery Targeting NS5 RNA- Dependent RNA Polymerase.

Curr Pharm Des 2020 May 23. Epub 2020 May 23.

Department of Chemistry, School of Science, GITAM (Deemed to be University), Hyderabad 502329, Telangana. India.

Dengue virus (DENV) infection threatens the health and wellbeing of almost 100 million people in the world. Vectored by mosquitoes, DENV may cause severe disease in human hosts called Dengue hemorrhagic fever (DHF)/Dengue shock syndrome (DSS), which are not preventable by any known drug. In the absence of a universally-accepted vaccine, a drug capable of inhibiting DENV multiplication is an urgent and unmet clinical need. Read More

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http://dx.doi.org/10.2174/1381612826666200523174753DOI Listing

Structural and molecular analyses of functional epitopes and escape mutants in Japanese encephalitis virus envelope protein domain III.

Authors:
Urmi Roy

Immunol Res 2020 May 22. Epub 2020 May 22.

Department of Chemistry & Biomolecular Science, Clarkson University, 8 Clarkson Avenue, Potsdam, NY, 13699-5820, USA.

The Japanese encephalitis virus (JEV) is one of the vector borne causes of encephalitis found in southeastern Asia. This positive single-stranded RNA virus is a member of the Flaviviridae family, which notably includes dengue, tick-borne, West Nile, Zika as well as yellow fever, and transmits to humans by infected mosquitos. The main site of interactions for antibodies against this virus is the envelope protein domain III (ED3). Read More

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http://dx.doi.org/10.1007/s12026-020-09130-yDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7243247PMC

Enhancing the Antiviral Efficacy of RNA-Dependent RNA Polymerase Inhibition by Combination with Modulators of Pyrimidine Metabolism.

Cell Chem Biol 2020 May 19. Epub 2020 May 19.

Department of Chemistry, Stanford University, Stanford, CA 94305, USA; Stanford Chemistry, Engineering and Medicine for Human Health (ChEM-H), Stanford University, Stanford, CA 94305, USA; Department of Chemical Engineering, Stanford University, Stanford, CA 94305, USA. Electronic address:

Genome-wide analysis of the mode of action of GSK983, a potent antiviral agent, led to the identification of dihydroorotate dehydrogenase as its target along with the discovery that genetic knockdown of pyrimidine salvage sensitized cells to GSK983. Because GSK983 is an ineffective antiviral in the presence of physiological uridine concentrations, we explored combining GSK983 with pyrimidine salvage inhibitors. We synthesized and evaluated analogs of cyclopentenyl uracil (CPU), an inhibitor of uridine salvage. Read More

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http://dx.doi.org/10.1016/j.chembiol.2020.05.002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7241336PMC

Super-Resolution Fluorescence Imaging Reveals That Serine Incorporator Protein 5 Inhibits Human Immunodeficiency Virus Fusion by Disrupting Envelope Glycoprotein Clusters.

ACS Nano 2020 Jun 1. Epub 2020 Jun 1.

Department of Pediatrics, Emory University School of Medicine, Atlanta, Georgia 30322, United States.

Serine incorporator protein 5 (SERINC5) is the host antiretroviral factor that reduces HIV-1 infectivity by incorporating into virions and inhibiting the envelope glycoprotein (Env) mediated virus fusion with target cells. We and others have shown that SERINC5 incorporation into virions alters the Env structure and sensitizes the virus to broadly neutralizing antibodies targeting cryptic Env epitopes. We have also found that SERINC5 accelerates the loss of Env function over time compared to control viruses. Read More

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http://dx.doi.org/10.1021/acsnano.0c02699DOI Listing

Ebola.

N Engl J Med 2020 05;382(19):1832-1842

From the Laboratory of Virology, Division of Intramural Research, National Institute of Allergy and Infectious Diseases, Rocky Mountain Laboratories, Hamilton, MT (H.F.); Médecins sans Frontières, Brussels (A.S.); and the Department of Microbiology and Immunology and Galveston National Laboratory, University of Texas Medical Branch at Galveston, Galveston (T.W.G.).

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http://dx.doi.org/10.1056/NEJMra1901594DOI Listing

Prioritisation of Anti-SARS-Cov-2 Drug Repurposing Opportunities Based on Plasma and Target Site Concentrations Derived from their Established Human Pharmacokinetics.

Clin Pharmacol Ther 2020 May 21. Epub 2020 May 21.

Department of Molecular and Clinical Pharmacology, Materials Innovation Factory, University of Liverpool, Liverpool, L7 3NY, UK.

There is a rapidly expanding literature on the in vitro antiviral activity of drugs that may be repurposed for therapy or chemoprophylaxis against SARS-CoV-2. However, this has not been accompanied by a comprehensive evaluation of the target plasma and lung concentrations of these drugs following approved dosing in humans. Accordingly, EC values recalculated from in vitro anti-SARS-CoV-2 activity data was expressed as a ratio to the achievable maximum plasma concentrations (Cmax) at an approved dose in humans (Cmax/EC ratio). Read More

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http://dx.doi.org/10.1002/cpt.1909DOI Listing

Structure of replicating SARS-CoV-2 polymerase.

Nature 2020 May 21. Epub 2020 May 21.

Max Planck Institute for Biophysical Chemistry, Department of Molecular Biology, Göttingen, Germany.

The coronavirus SARS-CoV-2 uses an RNA-dependent RNA polymerase (RdRp) for the replication of its genome and the transcription of its genes. Here we present the cryo-electron microscopic structure of the SARS-CoV-2 RdRp in active form, mimicking the replicating enzyme. The structure comprises the viral proteins nsp12, nsp8, and nsp7, and over two turns of RNA template-product duplex. Read More

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http://dx.doi.org/10.1038/s41586-020-2368-8DOI Listing

Tanshinones: An update in the medicinal chemistry in recent 5 years.

Curr Med Chem 2020 May 21. Epub 2020 May 21.

Institute of Drug Discovery and Design, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou. China.

Tanshinones is an important type of natural products isolated from Salvia miltiorrhiza Bunge with various bioactivities. Tanshinone IIa, cryptotanshinone and tanshinone I are three kinds of tanshinones which have been widely investigated. Particularly, sodium tanshinone IIa sulfonate is a water-soluble derivative of tanshinone IIa and it is used in clinical in China for treating cardiovascular diseases. Read More

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http://dx.doi.org/10.2174/0929867327666200521124850DOI Listing

Identification of 2-(4-(Phenylsulfonyl)piperazine-1-yl)pyrimidine Analogues as Novel Inhibitors of Chikungunya Virus.

ACS Med Chem Lett 2020 May 5;11(5):906-912. Epub 2020 Mar 5.

University of Vienna, Department of Pharmaceutical Chemistry, Althanstraße 14, A-1090 Vienna, Austria.

The chikungunya virus (CHIKV) is a mosquito-transmitted alphavirus, and it is the causative agent of chikungunya fever (CHIKF). Although it has re-emerged as an epidemic threat, so far there are neither vaccines nor pharmacotherapy available to prevent or treat an infection. Herein, we describe the synthesis and structure-activity relationship studies of a class of novel small molecule inhibitors against CHIKV and the discovery of a new potent inhibitor (compound ). Read More

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http://dx.doi.org/10.1021/acsmedchemlett.9b00662DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7236252PMC

5,6-Dihydroxypyrimidine Scaffold to Target HIV-1 Nucleocapsid Protein.

ACS Med Chem Lett 2020 May 19;11(5):766-772. Epub 2020 Mar 19.

Department of Biotechnology, Chemistry and Pharmacy, University of Siena, via Aldo Moro 2, 53100 Siena, Italy.

The HIV-1 nucleocapsid (NC) protein is a small basic DNA and RNA binding protein that is absolutely necessary for viral replication and thus represents a target of great interest to develop new anti-HIV agents. Moreover, the highly conserved sequence offers the opportunity to escape the drug resistance (DR) that emerged following the highly active antiretroviral therapy (HAART) treatment. On the basis of our previous research, nordihydroguaiaretic acid acts as a NC inhibitor showing moderate antiviral activity and suboptimal drug-like properties due to the presence of the catechol moieties. Read More

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http://dx.doi.org/10.1021/acsmedchemlett.9b00608DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7236274PMC

Bioassay-guided isolation of anti-hepatitis B virus flavonoid myricetin-3--rhamnoside along with quercetin from leaves.

Saudi Pharm J 2020 May 19;28(5):550-559. Epub 2020 Mar 19.

Department of Pharmaceutical Chemistry, Al-Neelain University, Khartoum, Sudan.

Recently, we have shown anti-hepatitis B virus (HBV) activity of J.F. Gmel leaves, and Identified quercetin and other flavonoids by HPTLC. Read More

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http://dx.doi.org/10.1016/j.jsps.2020.03.006DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7229332PMC

Challenges at the Time of COVID-19: Opportunities and Innovations in Antivirals from Nature.

Planta Med 2020 May 20. Epub 2020 May 20.

University Medicine Rostock, Chair of Complementary Medicine, Rostock, Germany.

As viral infections are an increasing threat to human societies, the need for new therapeutic strategies is becoming even more obvious. As no vaccine is available for COVID-19, the development of directly acting antiviral agents and preventive strategies have to be considered. Nature provides a huge reservoir of anti-infectious compounds, from which we can deduce innovative ideas, therapies, and products. Read More

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http://dx.doi.org/10.1055/a-1177-4396DOI Listing

Synthesis, Photophysical Properties, and Biological Profiling of Benzothieno-Fused 7-Deazapurine Ribonucleosides.

J Org Chem 2020 Jun 4. Epub 2020 Jun 4.

Department of Organic Chemistry, Faculty of Science, Charles University in Prague, Hlavova 8, CZ-12843 Prague 2, Czech Republic.

Two isomeric series of benzothieno-fused 7-deazapurine (benzo[4',5']thieno[3',2':4,5]- and benzo[4',5']thieno[2',3':4,5]pyrrolo[2,3-]pyrimidine) ribonucleosides were designed and synthesized. Key steps of the synthesis included the Negishi coupling of zincated dichloropyrimidine with 2- or 3-iodobenzothiophene followed by azidation, thermal or photochemical cyclization, glycosylation, and final functionalization at position 6 through cross-couplings or nucleophilic substitutions. Deprotection gave the final nucleosides, some of which showed moderate cytotoxic and antiviral activity. Read More

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http://dx.doi.org/10.1021/acs.joc.0c00927DOI Listing

Testosterone Protects Against Severe Influenza by Reducing the Pro-Inflammatory Cytokine Response in the Murine Lung.

Front Immunol 2020 22;11:697. Epub 2020 Apr 22.

Department Viral Zoonoses - One Health, Heinrich Pette Institute, Leibniz Institute for Experimental Virology, Hamburg, Germany.

Influenza A virus pathogenesis may differ between men and women. The 2009 H1N1 influenza pandemic resulted in more documented hospitalizations in women compared to men. In this study, we analyzed the impact of male sex hormones on pandemic 2009 H1N1 influenza A virus disease outcome. Read More

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http://dx.doi.org/10.3389/fimmu.2020.00697DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7216738PMC

Comparative Antiviral Activity of Remdesivir and Anti-HIV Nucleoside Analogs Against Human Coronavirus 229E (HCoV-229E).

Molecules 2020 May 17;25(10). Epub 2020 May 17.

Center for Targeted Drug Delivery, Department of Biomedical and Pharmaceutical Sciences, Chapman University School of Pharmacy, Harry and Diane Rinker Health Science Campus, Irvine, CA 92618, USA.

Remdesivir is a nucleotide prodrug that is currently undergoing extensive clinical trials for the treatment of COVID-19. The prodrug is metabolized to its active triphosphate form and interferes with the action of RNA-dependent RNA polymerase of SARS-COV-2. Herein, we report the antiviral activity of remdesivir against human coronavirus 229E (HCoV-229E) compared to known anti-HIV agents. Read More

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http://dx.doi.org/10.3390/molecules25102343DOI Listing
May 2020
2.416 Impact Factor

Deubiquitinating Enzymes in Coronaviruses and Possible Therapeutic Opportunities for COVID-19.

Int J Mol Sci 2020 May 15;21(10). Epub 2020 May 15.

Masonic Cancer Center and Department of Obstetrics, Gynecology and Women's Heath, University of Minnesota, Minneapolis, MN 55455, USA.

Following the outbreak of novel severe acute respiratory syndrome (SARS)-coronavirus (CoV)2, the majority of nations are struggling with countermeasures to fight infection, prevent spread and improve patient survival. Considering that the pandemic is a recent event, no large clinical trials have been possible and since coronavirus specific drug are not yet available, there is no strong consensus on how to treat the coronavirus disease 2019 (COVID-19) associated viral pneumonia. Coronaviruses code for an important multifunctional enzyme named papain-like protease (PLP), that has many roles in pathogenesis. Read More

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http://dx.doi.org/10.3390/ijms21103492DOI Listing

Thiosialoside-decorated polymers use a two-step mechanism to inhibit both early and late stages of influenza virus infection.

Eur J Med Chem 2020 Apr 28;199:112357. Epub 2020 Apr 28.

Key Laboratory of Industrial Microbiology, Ministry of Education, China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, College of Biotechnology, Tianjin University of Science & Technology, No. 29, 13th Avenue, TEDA, Tianjin, 300457, China; Research Centre of Modern Analytical Technology, Tianjin University of Science & Technology, No. 29, 13th Avenue, TEDA, Tianjin, 300457, China. Electronic address:

We describe the preparation of thiosialoside-modified poly (methyl vinyl ether-alt-maleic anhydride) as second-generation polymeric conjugates for the inhibition of influenza virus infection. These synthetic glycopolymers show significantly enhanced neuraminidase inhibitory and antiviral activity in enzyme and cellular levels, respectively. The polyvalent thiosialosides also exhibit comparable inhibitory activity to the first-line anti-influenza drugs Zanamivir® and Oseltamivir® against the PR8 influenza virus strain in virus growth inhibition assays, which may be attributed to multivalent binding to neuraminidase on the virion particles, leading to the virion aggregation and further inhibiting the attaching/fusion and releasing steps in the influenza virus life-cycle. Read More

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http://dx.doi.org/10.1016/j.ejmech.2020.112357DOI Listing
April 2020
3.447 Impact Factor

Isolation and Identification of Three New Sterigmatocystin Derivatives from the Fungus Aspergillus versicolor Guided by Molecular Networking Approach.

Chem Biodivers 2020 May 19. Epub 2020 May 19.

Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao, 266003, P. R. China.

Molecular networking approach was applied for the targeted isolation of new sterigmatocystin derivatives, sterigmatocystins A-C, from the marine sponge-derived fungus Aspergillus versicolor. Sterigmatocystin A features a rare 6/6/6/6/5 polycyclic system. The structures of sterigmatocystins A-C, including absolute configurations, were determined on the basis of spectroscopic data and ECD calculations. Read More

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http://dx.doi.org/10.1002/cbdv.202000208DOI Listing

Zinc oxide nanoparticles for therapeutic purposes in cancer medicine.

J Mater Chem B 2020 May 19. Epub 2020 May 19.

Department of Otorhinolaryngology, Head and Neck Surgery, University Medical Centre of the Johannes Gutenberg-University, Laboratory for Molecular Tumor Biology, Langenbeckstraße 1, 55131 Mainz, Germany.

The importance of zinc as a trace metal in the human body has long been overlooked. We now gradually discover that the impact of zinc on the health of our body might be as far-reaching as that of iron. Concurrently, nanomaterials containing zinc, in particular zinc oxide nanoparticles (ZnO NPs), are becoming increasingly attractive as innovative agents for medical applications. Read More

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http://dx.doi.org/10.1039/d0tb00739kDOI Listing

Antiviral Peptides: Identification and Validation.

Int J Pept Res Ther 2020 May 18:1-20. Epub 2020 May 18.

Department of Biotechnology, Center for Emerging Diseases, Jaypee Institute of Information Technology, Noida, UP 201309 India.

Despite rapid advances in the human healthcare, the infection caused by certain viruses results in high morbidity and mortality accentuate the importance for development of new antivirals. The existing antiviral drugs are limited, due to their inadequate response, increased rate of resistance and several adverse side effects. Therefore, one of the newly emerging field "peptide-based therapeutics" against viruses is being explored and seems promising. Read More

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http://dx.doi.org/10.1007/s10989-020-10072-0DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7233194PMC

Triterpenoids From Species: Phytochemistry, Structure Modification, and Bioactivities.

Front Chem 2020 30;8:363. Epub 2020 Apr 30.

Tianjin Key Laboratory of TCM Chemistry and Analysis, Institute of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, China.

Plants from species belong to the genus of Linn. in family. The tubers of (Sam. Read More

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http://dx.doi.org/10.3389/fchem.2020.00363DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7205456PMC

Characterization of Novel Aptamers Specifically Directed to Red-Spotted Grouper Nervous Necrosis Virus (RGNNV)-Infected Cells for Mediating Targeted siRNA Delivery.

Front Microbiol 2020 30;11:660. Epub 2020 Apr 30.

Guangdong Laboratory for Lingnan Modern Agriculture, College of Marine Sciences, South China Agricultural University, Guangzhou, China.

Nervous necrosis virus (NNV) causes viral nervous necrosis, the most devastating disease in more than 50 fish species worldwide, with massive mortality rates up to 100%, resulting in great economic losses to mariculture. However, few methods are available for the efficient diagnosis and treatment of viral nervous necrosis. Aptamers are molecular recognition ligands characterized by their remarkably high specificity and affinity, great stability, and ease of synthesis, and have been widely studied in application of disease diagnosis and therapies. Read More

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http://dx.doi.org/10.3389/fmicb.2020.00660DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7203557PMC

An overview of COVID-19.

J Zhejiang Univ Sci B 2020 May 8;21(5):343-360. Epub 2020 May 8.

State Key Laboratory for Diagnosis and Treatment of Infectious Diseases, National Clinical Research Center for Infectious Diseases, Collaborative Innovation Center for Diagnosis and Treatment of Infectious Diseases, the First Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou 310003, China.

Pneumonia caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection emerged in Wuhan City, Hubei Province, China in December 2019. By Feb. 11, 2020, the World Health Organization (WHO) officially named the disease resulting from infection with SARS-CoV-2 as coronavirus disease 2019 (COVID-19). Read More

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http://dx.doi.org/10.1631/jzus.B2000083DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7205601PMC

Remdesivir in adults with severe COVID-19: a randomised, double-blind, placebo-controlled, multicentre trial.

Lancet 2020 05 29;395(10236):1569-1578. Epub 2020 Apr 29.

Department of Pulmonary and Critical Care Medicine, Center of Respiratory Medicine, National Clinical Research Center for Respiratory Diseases, China-Japan Friendship Hospital, Beijing, China; Institute of Respiratory Medicine, Chinese Academy of Medical Science, Beijing, China; Tsinghua University-Peking University Joint Center for Life Sciences, Beijiing, China; Peking Union Medical College, Beijing, China. Electronic address:

Background: No specific antiviral drug has been proven effective for treatment of patients with severe coronavirus disease 2019 (COVID-19). Remdesivir (GS-5734), a nucleoside analogue prodrug, has inhibitory effects on pathogenic animal and human coronaviruses, including severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in vitro, and inhibits Middle East respiratory syndrome coronavirus, SARS-CoV-1, and SARS-CoV-2 replication in animal models.

Methods: We did a randomised, double-blind, placebo-controlled, multicentre trial at ten hospitals in Hubei, China. Read More

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http://dx.doi.org/10.1016/S0140-6736(20)31022-9DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7190303PMC
May 2020
45.217 Impact Factor