39,557 results match your criteria Antiviral Chemistry & Chemotherapy[Journal]


Identification of small molecule inhibitors targeting the Zika virus envelope protein.

Antiviral Res 2019 Feb 13. Epub 2019 Feb 13.

Department of Microbiology and Blavatnik Institute, Harvard Medical School, 77 Avenue Louis Pasteur, Boston, MA 02115, USA. Electronic address:

The recent emergence of Zika virus, a mosquito-borne flavivirus, in the Americas has shed light on the severe neurological diseases associated with infection, notably congenital microcephaly in newborns and Guillain-Barré syndrome in adults. Despite the recent focus on Zika virus, there are currently no approved vaccines or antiviral therapies available to treat or prevent infection. In this study we established a competitive amplified luminescent proximity homogeneous assay (ALPHAscreen) to identify small molecule inhibitors targeting the envelope protein of Zika virus (Zika E). Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.antiviral.2019.02.008DOI Listing
February 2019
1 Read

Iron oxide nanoparticles based antiviral activity of H1N1 influenza A virus.

J Infect Chemother 2019 Feb 12. Epub 2019 Feb 12.

Molecular Biology Department, Rajendra Memorial Research Institute of Medical Sciences (ICMR), Patna, India. Electronic address:

Influenza virus is a common human pathogenic agent that has caused serious respiratory illness and death over the past century and in recent year. Treatment options against pandemic influenza strain A/H1N1 are very limited and unsatisfactory. Therefore we have developed iron oxide nanoparticles (IO-NPs) with particle size in the range of 10-15 nm against pandemic influenza strain A/H1N1/Eastern India/66/PR8-H1N1. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.jiac.2018.12.006DOI Listing
February 2019

Update: Influenza Activity - United States, September 30, 2018-February 2, 2019.

MMWR Morb Mortal Wkly Rep 2019 Feb 15;68(6):125-134. Epub 2019 Feb 15.

Influenza Division, National Center for Immunization and Respiratory Diseases, CDC.

CDC collects, compiles, and analyzes data on influenza activity and viruses in the United States. During September 30, 2018-February 2, 2019,* influenza activity in the United States was low during October and November, increased in late December, and remained elevated through early February. As of February 2, 2019, this has been a low-severity influenza season (1), with a lower percentage of outpatient visits for influenza-like illness (ILI), lower rates of hospitalization, and fewer deaths attributed to pneumonia and influenza, compared with recent seasons. Read More

View Article

Download full-text PDF

Source
http://www.cdc.gov/mmwr/volumes/68/wr/mm6806a1.htm?s_cid=mm6
Publisher Site
http://dx.doi.org/10.15585/mmwr.mm6806a1DOI Listing
February 2019
1 Read

Chemistry, Alpha-glucosidase and Radical Scavenging Properties of Uranyl(VI) Hydrazide Complexes.

Med Chem 2019 Feb 12. Epub 2019 Feb 12.

Department of Chemistry, University of Karachi, Karachi 75270. Pakistan.

Background: Antioxidant, anti-inflammatory, antiviral and antitumoral activities among others are essential characteristics in the development of novel therapeutic compounds. Acid hydrazides can form complexation with certain metal ions that positively enhances these biological characteristics.

Objective: Five new complexes of uranium with hydrazide ligands were synthesized at room temperature. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.2174/1573406415666190213101044DOI Listing
February 2019

Infectious complications and NK cell depletion following daratumumab treatment of Multiple Myeloma.

PLoS One 2019 13;14(2):e0211927. Epub 2019 Feb 13.

Division of Hematology, Department of Medicine Huddinge, Karolinska Institutet, Stockholm, Sweden.

Treatment with Daratumumab (Dara), a monoclonal anti-CD38 antibody of IgG1 subtype, is effective in patients with multiple myeloma (MM). However, Dara also impairs the cellular immunity, which in turn may lead to higher susceptibility to infections. The exact link between immune impairment and infectious complications is unclear. Read More

View Article

Download full-text PDF

Source
http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0211927PLOS
February 2019

Enhanced taxonomy annotation of antiviral activity data from ChEMBL.

Database (Oxford) 2019 Jan 1;2019. Epub 2019 Jan 1.

FSBSI "Chumakov FSC R&D IBP RAS", Moscow, Russia.

The discovery of antiviral drugs is a rapidly developing area of medicinal chemistry research. The emergence of resistant variants and outbreaks of poorly studied viral diseases make this area constantly developing. The amount of antiviral activity data available in ChEMBL consistently grows, but virus taxonomy annotation of these data is not sufficient for thorough studies of antiviral chemical space. Read More

View Article

Download full-text PDF

Source
https://academic.oup.com/database/article/doi/10.1093/databa
Publisher Site
http://dx.doi.org/10.1093/database/bay139DOI Listing
January 2019
1 Read

Synthesis of d-(+)-camphor-based -acylhydrazones and their antiviral activity.

Medchemcomm 2018 Dec 26;9(12):2072-2082. Epub 2018 Oct 26.

Novosibirsk Institute of Organic Chemistry , Siberian Branch of the Russian Academy of Sciences , Lavrentjev Ave. 9 , 630090 Novosibirsk , Russian Federation . Email:

The design and synthesis of a series of novel d-(+)-camphor -acylhydrazones exhibiting inhibitory activity against vaccinia and influenza viruses are presented. An easy pathway to camphor-based -acylhydrazones containing in their structure aliphatic, aromatic, and heterocyclic pharmacophore scaffolds has been developed. The conformation and configuration of the synthesized hydrazones were thoroughly characterized by a complete set of spectral characterization techniques, including 2D NMR spectroscopy, mass spectrometry, and X-ray diffraction analysis. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1039/c8md00442kDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6335999PMC
December 2018

Novel influenza inhibitors designed to target PB1 interactions with host importin RanBP5.

Antiviral Res 2019 Feb 8. Epub 2019 Feb 8.

Department of Physiology and Developmental Biology, Brigham Young University, Provo, UT 84602, USA. Electronic address:

In search of novel targets for influenza inhibitors, a site on PB1 was selected for its high conservation and probable interaction with a host protein, RanBP5, that is key to nuclear import of PB1, where it complexes with PB2, PA, and NP to transcribe viral RNA. Docking with libraries of drug-like compounds led to a selection of five candidates that bound tightly and with a pose likely to inhibit protein binding. These were purchased and tested in vitro, found to be active, and then one was synthetically expanded to explore the structure-activity relationship. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.antiviral.2019.02.003DOI Listing
February 2019

An overview of grayanane diterpenoids and their biological activities from the Ericaceae family in the last seven years.

Eur J Med Chem 2019 Feb 1;166:400-416. Epub 2019 Feb 1.

Shaanxi Key Laboratory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A & F University, Yangling, 712100, Shaanxi, People's Republic of China. Electronic address:

Grayanane diterpenoids, possessing a unique 5/7/6/5 tetracyclic system, exist exclusively in plants of the Ericaceae family. Owing to their various skeletons, complex structures, and diverse bioactivities, grayanoids have been the topic of research in many phytochemical and pharmacological laboratories, offering opportunities for the development of new drugs with analgesic, anti-inflammatory, and protein tyrosine phosphatase 1B (PTP1B) properties. Recently, a number of new grayanane diterpenoids with unprecedented carbon skeletons have been obtained from plants of the Ericaceae family, and they exhibit diverse biological properties, such as agalgesic, antinociceptive, anticancer, antiviral, antifeedant, insecticidal, toxicity, and PTP1B. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejmech.2019.01.079DOI Listing
February 2019

Synthesis and anti-HSV activity of tricyclic penciclovir and hydroxybutylguanine derivatives.

Bioorg Med Chem 2019 Feb 2. Epub 2019 Feb 2.

School of Pharmacy & Pharmaceutical Sciences, Cardiff University, King Edward VII Avenue, Cardiff CF10 3NB, UK. Electronic address:

A series of tricyclic penciclovir (PCV) and hydroxybutylguanine (HBG) derivatives have been prepared with enhanced lipophilicity following an efficient synthetic route. All the novel tricyclic derivatives were evaluated for inhibitory activity against herpes simplex virus 1 and 2 (HSV-1, HSV-2) and thymidine kinase deficient (ACV resistant) HSV-1. The tricyclic HBG derivatives were devoid of inhibitory activity however several of the tricyclic PCV derivatives showed promising antiviral activity, in particular 9g (R = 4-MeO-CH) displayed good inhibitory activity (HSV-1 EC 1. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmc.2019.02.005DOI Listing
February 2019
1 Read

The antiviral activity and cytotoxicity of 15 natural phenolic compounds with previously demonstrated antifungal activity.

J Environ Sci Health B 2019 Feb 8:1-7. Epub 2019 Feb 8.

a Center for Genic and Cellular Therapies in Cancer Treatment , Timisoara , Romania.

The present study attempted to evaluate the carcinogenicity of natural phenolic compounds with previously demonstrated antifungal activity, using a computational structure-cytotoxicity approach, namely the quantum structure cytotoxicity relationship model. The cytotoxicity of 15 phenolic compounds with antiviral activity 96 h after treatment was studied using the AdmetSAR computational program. Per the EPA classification, four of the investigated compounds would be included in the second cytotoxicity category, four in the third category, and six showed no toxicity, rendering the studied natural phenolic compounds much less toxic to aquatic life than synthetic pesticides, the organophosphorus compounds, which mostly fall into the first and second categories of toxicity. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1080/03601234.2019.1574176DOI Listing
February 2019

Natural Products for Drug Discovery: Discovery of Gramines as Novel Agents against a Plant Virus.

J Agric Food Chem 2019 Feb 15. Epub 2019 Feb 15.

State Key Laboratory of Elemento-Organic Chemistry, Research Institute of Elemento-Organic Chemistry, College of Chemistry, Collaborative Innovation Center of Chemical Science and Engineering (Tianjin) , Nankai University , Tianjin 300071 , China.

Plant viral diseases seriously affect crop yield and quality. The natural product gramine (1) and its simple structural analogues 2-35 were synthesized from indoles, amines, and aldehydes in one step. The antiviral effects of these alkaloids were evaluated systematically. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.jafc.8b06859DOI Listing
February 2019
1 Read

Computational screening of medicinal plant phytochemicals to discover potent pan-serotype inhibitors against dengue virus.

Sci Rep 2019 Feb 5;9(1):1433. Epub 2019 Feb 5.

Department of Biosciences, COMSATS University Islamabad, Islamabad, Pakistan.

Emergence of Dengue as one of the deadliest viral diseases prompts the need for development of effective therapeutic agents. Dengue virus (DV) exists in four different serotypes and infection caused by one serotype predisposes its host to another DV serotype heterotypic re-infection. We undertook virtual ligand screening (VLS) to filter compounds against DV that may inhibit inclusively all of its serotypes. Read More

View Article

Download full-text PDF

Source
http://www.nature.com/articles/s41598-018-38450-1
Publisher Site
http://dx.doi.org/10.1038/s41598-018-38450-1DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6363786PMC
February 2019
3 Reads

A Short Chemically Modified dsRNA-Binding PNA (dbPNA) Inhibits Influenza Viral Replication by Targeting Viral RNA Panhandle Structure.

Bioconjug Chem 2019 Feb 15. Epub 2019 Feb 15.

Institute of Bioorganic Chemistry, Polish Academy of Sciences , Noskowskiego 12/14 , 61-704 Poznan , Poland.

RNAs play critical roles in diverse catalytic and regulatory biological processes and are emerging as important disease biomarkers and therapeutic targets. Thus, developing chemical compounds for targeting any desired RNA structures has great potential in biomedical applications. The viral and cellular RNA sequence and structure databases lay the groundwork for developing RNA-binding chemical ligands through the recognition of both RNA sequence and RNA structure. Read More

View Article

Download full-text PDF

Source
http://pubs.acs.org/doi/10.1021/acs.bioconjchem.9b00039
Publisher Site
http://dx.doi.org/10.1021/acs.bioconjchem.9b00039DOI Listing
February 2019
1 Read

Mobility-Based Quantification of Multivalent Virus-Receptor Interactions: New Insights Into Influenza A Virus Binding Mode.

Nano Lett 2019 Feb 13. Epub 2019 Feb 13.

Department of Chemistry and Biochemistry, Emmy-Noether Group "Bionanointerfaces" , Freie Universität Berlin , Takustrasse 3 , 14195 Berlin , Germany.

Viruses, such as influenza A, typically bind to the plasma membrane of their host by engaging multiple membrane receptors in parallel, thereby forming so-called multivalent interactions that are created by the collective action of multiple weak ligand-receptor bonds. The overall interaction strength can be modulated by changing the number of engaged receptors. This feature is used by viruses to achieve a sufficiently firm attachment to the host's plasma membrane but also allows progeny viruses to leave the plasma membrane after completing the virus replication cycle. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.nanolett.8b04969DOI Listing
February 2019

A Massively Parallel Selection of Small Molecule-RNA Motif Binding Partners Informs Design of an Antiviral from Sequence.

Chem 2018 Oct 13;4(10):2384-2404. Epub 2018 Sep 13.

Department of Chemistry, The Scripps Research Institute, Jupiter, FL 33458, USA.

Many RNAs cause disease; however, RNA is rarely exploited as a small-molecule drug target. Our programmatic focus is to define privileged RNA motif small-molecule interactions to enable the rational design of compounds that modulate RNA biology starting from only sequence. We completed a massive, library-versus-library screen that probed over 50 million binding events between RNA motifs and small molecules. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.chempr.2018.08.003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6358276PMC
October 2018
1 Read

Successes, failures, and future prospects of prodrugs and their clinical impact.

Expert Opin Drug Discov 2019 Feb 4:1-22. Epub 2019 Feb 4.

a Department of Bioorganic & Pharmaceutical Chemistry, Faculty of Pharmacy , Al-Quds University , Jerusalem , Palestine.

Introduction: Ample efforts have been carried out to improve the efficacy of a variety of drugs. The prodrugs approach was found to be a safe haven for providing medications with improved pharmacokinetic and pharmacodynamic properties. Areas covered: Herein, several selected successful prodrugs are reported and categorized. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1080/17460441.2019.1567487DOI Listing
February 2019
3.467 Impact Factor

Mechanism of action of an old antibiotic revisited: Role of calcium ions in protonophoric activity of usnic acid.

Biochim Biophys Acta Bioenerg 2019 Jan 30;1860(4):310-316. Epub 2019 Jan 30.

Belozersky Institute of Physico-Chemical Biology, Lomonosov Moscow State University, 119991 Moscow, Russia.

Usnic acid (UA), an old antibiotic and one of the first described mitochondrial uncouplers, has demonstrated many beneficial activities, such as antimicrobial, antiviral, antitumour and anti-inflammatory properties. Here, we performed a thorough investigation of effects of usnic acid and its analogues on artificial planar bilayer lipid membrane (BLM), rat liver mitochondria and bacteria. Surprisingly enough, all of the three hydroxyl groups of UA appeared to be involved in its proton-shuttling activity on BLM. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bbabio.2019.01.005DOI Listing
January 2019

Chikungunya virus inhibition by synthetic coumarin-guanosine conjugates.

Eur J Med Chem 2019 Jan 21;166:136-143. Epub 2019 Jan 21.

Department of Chemistry, National Tsing Hua University, Hsinchu, 300, Taiwan; Frontier Research Center on Fundamental and Applied Sciences of Matters, National Tsing Hua University, Hsinchu, 300, Taiwan; Department of Chemistry, National Central University, Jhongli City, Taoyuan, 320, Taiwan. Electronic address:

Since its discovery in Tanganyika, Africa in 1952, chikungunya virus (CHIKV) outbreaks have occurred in Africa, Asia, Europe, and America. Till now chikungunya fever has spread in nearly 40 countries. Because of lack of effective vaccines and antiviral drugs to intervene this disease, 21 new conjugated compounds were designed and synthesized by coupling of 6,8-dithioguanosine at its C-6 position with 3-(chloromethyl)coumarins bearing an F, Cl, Br, Me, or -OMe substituent through the -SCH- joint. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S02235234193004
Publisher Site
http://dx.doi.org/10.1016/j.ejmech.2019.01.037DOI Listing
January 2019
4 Reads

pH Controlled Intersystem Crossing and Singlet Oxygen Generation of 8-Azaadenine in Aqueous Solution.

Chemphyschem 2019 Jan 31. Epub 2019 Jan 31.

State Key Laboratory of Precision Spectroscopy, East China Normal University, Shanghai, 200062, China.

Azabases are intriguing DNA and RNA analogues and have been used as effective antiviral and anticancer medicines. However, photosensitivity of these drugs has also been reported. Here, pH-controlled intersystem crossing (ISC) process of 9H 8-azaadenine (8-AA) in aqueous solution is reported. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1002/cphc.201800969DOI Listing
January 2019
3.419 Impact Factor

Characterization of ssDNA aptamers specifically directed against Trachinotus ovatus NNV (GTONNV)-infected cells with antiviral activities.

J Gen Virol 2019 Jan 30. Epub 2019 Jan 30.

3​Guangxi Laboratory on the Study of Coral Reefs in the South China Sea, College of Marine Sciences, Guangxi University, Nanning, PR China.

Nervous necrosis virus (NNV), is one of the most fatal viruses in marine fish aquaculture, and is capable of infecting over 50 different fish species. Trachinotus ovatus NNV (GTONNV) was isolated from diseased golden pompano. This T. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1099/jgv.0.001226DOI Listing
January 2019

Glycosaminoglycan Compositional Analysis of Relevant Tissues in Zika Virus Pathogenesis and in Vitro Evaluation of Heparin as an Antiviral against Zika Virus Infection.

Biochemistry 2019 Feb 13. Epub 2019 Feb 13.

Biochemistry and Biophysics Graduate Program, Center for Biotechnology and Interdisciplinary Studies , Rensselaer Polytechnic Institute , Troy , New York 12180 , United States.

Zika virus (ZIKV) is an enveloped RNA virus from the flavivirus family that can cause fetal neural abnormalities in pregnant women. Previously, we established that ZIKV-EP (envelope protein) binds to human placental chondroitin sulfate (CS), suggesting that CS may be a potential host cell surface receptor in ZIKV pathogenesis. In this study, we further characterized the GAG disaccharide composition of other biological tissues (i. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.biochem.8b01267DOI Listing
February 2019

Recombinant HCV NS3 and NS5B enzymes exhibit multiple posttranslational modifications for potential regulation.

Virus Genes 2019 Jan 29. Epub 2019 Jan 29.

Fundación Ciencia &, Vida, Avda. Zañartu 1482, 7780272, Ñuñoa, Santiago, Chile.

Posttranslational modification (PTM) of proteins is critical to modulate protein function and to improve the functional diversity of polypeptides. In this report, we have analyzed the PTM of both hepatitis C virus NS3 and NS5B enzyme proteins, upon their individual expression in insect cells under the baculovirus expression system. Using mass spectrometry, we present evidence that these recombinant proteins exhibit diverse covalent modifications on certain amino acid side chains, such as phosphorylation, ubiquitination, and acetylation. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s11262-019-01638-2DOI Listing
January 2019

The synthesis of monodisperse silver nanoparticles with plant extracts.

Colloids Surf B Biointerfaces 2019 Jan 22;177:19-24. Epub 2019 Jan 22.

Department of Materials Technology and Chemistry, Faculty of Chemistry, University of Lodz, Pomorska 163, 90-236 Lodz, Poland. Electronic address:

Plant extracts are known for their antihyperglycemic, antioxidant, antimutagenic, antifungal, anti-inflammatory, antiviral and antibacterial properties. These biological properties make plant extracts interesting surface modifiers of nanoparticles (NPs), which are also known for their unique features. Plant extracts can play a multifunctional role in the synthesis of NPs (i. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.colsurfb.2019.01.037DOI Listing
January 2019

Mechanical characterization and ex vivo evaluation of anticancer and antiviral drug printed bioadhesive film for the treatment of cervical cancer.

Eur J Pharm Sci 2019 Jan 25;130:114-123. Epub 2019 Jan 25.

Department of Pharmaceutical Technology, Faculty of Pharmacy, Hacettepe University, 06100, Sıhhiye, Ankara, Turkey.

As research progresses on personalized medicines, it is clear that personalized and flexible formulations can provide effective treatment with reduced side effects especially for diseases like cancer, characteristic of high patient variability. 2D and 3D printers are frequently reported in the literature for the preparation of pharmaceutical products with adjusted dose and selected drug combinations. However, in-depth characterization studies of these formulations are rather limited. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejps.2019.01.030DOI Listing
January 2019
1 Read

Rhodium catalyzed stereospecific reductive carbocyclization of 1,6-enynes and synthesis of 4'-methyl-6'-substituted aristeromycins.

Nucleosides Nucleotides Nucleic Acids 2019 Jan 28:1-9. Epub 2019 Jan 28.

b Department of Chemistry , Birla Institute of Technology , Ranchi , Jharkhand , India.

The need of long-term treatment for chronic HBV, emergence of drug-resistant viruses and inefficiency of currently approved therapies to eliminate covalently closed circular DNA (cccDNA), mandates identification of potent and selective inhibitors of HBV replication with novel mechanisms of action. Entecavir, a carbocyclic guanosine nucleoside analog, is the most potent inhibitor of HBV replication on the market. Moreover, the naturally occurring carbocyclic nucleosides aristeromycin are known for their wide range of antiviral activities. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1080/15257770.2018.1554221DOI Listing
January 2019

Synthesis of New Hydrazone Derivatives and Evaluation of their Efficacy as Proliferation Inhibitors in Human Cancer Cells.

Med Chem 2019 Jan 27. Epub 2019 Jan 27.

Department of Molecular and Cellular Biology, Wroclaw Medical University, Borowska 211A, 50-556 Wroclaw. Poland.

Background: Hydrazine-hydrazones represent a group of bioactive compounds that display antibacterial, anti-inflammatory, antiviral or anticancer activities.

Objective: In this study, we designed new derivative compounds from groups of hydrazones.

Method: The group of new derivatives was evaluated by the viability assay in human cancer and normal cells. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.2174/1573406415666190128100524DOI Listing
January 2019
2 Reads

Aminoalkoxyfluorenones and aminoalkoxybiphenyls: DNA binding modes.

Bioorg Chem 2019 Jan 16;86:52-60. Epub 2019 Jan 16.

Department of Pharmaceutical Sciences, School of Pharmacy, Hampton University, Kittrell Hall, Hampton, VA 23668, USA. Electronic address:

Many evidences suggest that DNA-drug interaction in the minor groove and the intercalation of drugs into DNA may play critical roles in antiviral, antimicrobial, and antitumor activities. As a continuous effort to develop novel antiviral agents, the series of planar fluorenone (3a-7d) were synthesized and used along with nonplanar biphenyls (11a-d) for the comparative analysis of their interaction with DNA. The chemical structure of new compounds was confirmed by H NMR, C NMR and mass spectra as well as elemental analysis. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bioorg.2019.01.024DOI Listing
January 2019
1 Read

Spectrophotometric assessment of the brand new antiviral combination: Sofosbuvir and velpatasvir in their pure forms and pharmaceutical formulation.

Spectrochim Acta A Mol Biomol Spectrosc 2019 Jan 16;213:159-166. Epub 2019 Jan 16.

Analytical Chemistry Department, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, 11562 Cairo, Egypt. Electronic address:

Sofosbuvir (SOF) and velpatasvir (VEL) are recently co-formulated together for the treatment of hepatitis C virus. Smart and robust spectrophotometric methods were first developed and validated for quantification of SOF and VEL in their pure forms and in their combined pharmaceutical formulation without preliminary separation. VEL has two UV maxima at 302. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.saa.2019.01.058DOI Listing
January 2019
2 Reads

Antiviral activity spectrum of phenoxazine nucleoside derivatives.

Antiviral Res 2019 Mar 23;163:117-124. Epub 2019 Jan 23.

Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Moscow 117997, Russia. Electronic address:

The phenoxazine scaffold is widely used to stabilize nucleic acid duplexes, as a part of fluorescent probes for the study of nucleic acid structure, recognition, and metabolism, etc. Here we present the synthesis of phenoxazine-based nucleoside derivatives and their antiviral activity against a panel of structurally diverse viruses: enveloped DNA herpesviruses varicella zoster virus (VZV) and human cytomegalovirus, enveloped RNA tick-borne encephalitis virus (TBEV), and non-enveloped RNA enteroviruses. Studied compounds were effective against DNA and RNA viruses reproduction in cell culture. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.antiviral.2019.01.010DOI Listing
March 2019
2 Reads

Discovery of Pimprinine Alkaloids as Novel Agents against a Plant Virus.

J Agric Food Chem 2019 Feb 6. Epub 2019 Feb 6.

State Key Laboratory of Elemento-Organic Chemistry, Research Institute of Elemento-Organic Chemistry, College of Chemistry, Collaborative Innovation Center of Chemical Science and Engineering (Tianjin) , Nankai University , Tianjin 300071 , China.

Plant viral diseases cause tremendous decreases in crop yield and quality. Natural products have always been a valuable source for lead discovery in medicinal and agricultural chemistry. A series of pimprinine alkaloids and their derivatives were prepared and identified by nuclear magnetic resonance (NMR) spectroscopy and high-resolution mass spectrometry (HR-MS). Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.jafc.8b06175DOI Listing
February 2019
1 Read

A study of affecting the recovery of Chinese patients with Bell palsy.

Medicine (Baltimore) 2019 Jan;98(4):e14244

College of Basic Medical Science, Zhejiang Chinese Medical University, Hangzhou, China.

We explored the risk factors for preventing recovery of Bell palsy (BP) in Chinese inpatients. Five hundred thirteen patients were included. The two end-points of assessment were the discharge and final follow-up results. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1097/MD.0000000000014244DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6358322PMC
January 2019
1 Read

Design, synthesis and characterization of new macrocyclic inhibitors of the proprotein convertase furin.

ChemMedChem 2019 Jan 25. Epub 2019 Jan 25.

Philipps-University Marburg, Institute of Pharmaceutical Chemistry, Marbacher Weg 6, 35032, Marburg, GERMANY.

The activation of viral glycoproteins by the host protease furin is an essential step in the replication of numerous pathogenic viruses. Thus, effective inhibitors of furin could serve as broad-spectrum antiviral drugs. A crystal structure of an inhibitory hexapeptide derivative in complex with furin served as template for the rational design of various types of new cyclic inhibitors. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1002/cmdc.201800807DOI Listing
January 2019
1 Read

Dynamics and binding interactions of peptide inhibitors of dengue virus entry.

J Biol Phys 2019 Jan 24. Epub 2019 Jan 24.

Department of Chemistry, Faculty of Science, University of Malaya, 50603, Kuala Lumpur, Malaysia.

In this study, we investigate the binding interactions of two synthetic antiviral peptides (DET2 and DET4) on type II dengue virus (DENV2) envelope protein domain III. These two antiviral peptides are designed based on the domain III of the DENV2 envelope protein, which has shown significant inhibition activity in previous studies and can be potentially modified further to be active against all dengue strains. Molecular docking was performed using AutoDock Vina and the best-ranked peptide-domain III complex was further explored using molecular dynamics simulations. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s10867-018-9515-6DOI Listing
January 2019

Thioguanine-based DENV-2 NS2B/NS3 protease inhibitors: Virtual screening, synthesis, biological evaluation and molecular modelling.

PLoS One 2019 24;14(1):e0210869. Epub 2019 Jan 24.

School of Pharmaceutical Sciences, Universiti Sains Malaysia, Minden, Pulau Pinang, Malaysia.

Dengue virus Type 2 (DENV-2) is predominant serotype causing major dengue epidemics. There are a number of studies carried out to find its effective antiviral, however to date, there is still no molecule either from peptide or small molecules released as a drug. The present study aims to identify small molecules inhibitor from National Cancer Institute database through virtual screening. Read More

View Article

Download full-text PDF

Source
http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0210869PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6345492PMC
January 2019

Iridoid, phenylethanoid and flavonoid glycosides from Forsythia suspensa.

Nat Prod Res 2019 Jan 24:1-6. Epub 2019 Jan 24.

a Department of Medicinal Chemistry and Natural Medicine Chemistry , College of Pharmacy, HarBin Medical University , HarBin , People's Republic of China.

As part of our continuing efforts to explore bioactive compounds from natural resources, a new iridoid glycoside, adoxosidic acid-6'-oleuroperic ester (1), together with one known phenylethanoid glycoside (2) and two known flavonoid glycosides (3-4) were isolated from the fruit of Forsythia suspensa. The structure of the new compound (1) was elucidated through 1D and 2D NMR spectroscopic data and HR-ESIMS. Interestingly, compound 1 was a monoterpene ester of one iridoid glycoside. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1080/14786419.2018.1560288DOI Listing
January 2019

Validating Enterovirus D68-2A as an Antiviral Drug Target and the Discovery of Telaprevir as a Potent D68-2A Inhibitor.

J Virol 2019 Jan 23. Epub 2019 Jan 23.

Department of Pharmacology and Toxicology, College of Pharmacy, The University of Arizona, Tucson, USA

Enterovirus D68 (EV-D68) is a viral pathogen that leads to severe respiratory illness and has been linked with the development of acute flaccid myelitis (AFM) in children. No vaccines or antivirals are currently available for EV-D68 infection, and treatment options for hospitalized patients are limited to supportive care. Here, we report the expression of the EV-D68 2A protease (2A) and characterization of its enzymatic activity. Read More

View Article

Download full-text PDF

Source
http://jvi.asm.org/lookup/doi/10.1128/JVI.02221-18
Publisher Site
http://dx.doi.org/10.1128/JVI.02221-18DOI Listing
January 2019
9 Reads

Zika Virus Dependence on Host Hsp70 Provides a Protective Strategy against Infection and Disease.

Cell Rep 2019 Jan;26(4):906-920.e3

Department of Biology and Genetics, Stanford University, Stanford, CA 94305, USA. Electronic address:

The spread of mosquito-borne Zika virus (ZIKV), which causes neurological disorders and microcephaly, highlights the need for countermeasures against sudden viral epidemics. Here, we tested the concept that drugs targeting host proteostasis provide effective antivirals. We show that different cytosolic Hsp70 isoforms are recruited to ZIKV-induced compartments and are required for virus replication at pre- and post-entry steps. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.celrep.2018.12.095DOI Listing
January 2019
1 Read

Double-Stranded RNA Sensors and Modulators in Innate Immunity.

Authors:
Sun Hur

Annu Rev Immunol 2019 Jan 23. Epub 2019 Jan 23.

Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, Massachusetts 02115, USA; email:

Detection of double-stranded RNAs (dsRNAs) is a central mechanism of innate immune defense in many organisms. We here discuss several families of dsRNA-binding proteins involved in mammalian antiviral innate immunity. These include RIG-I-like receptors, protein kinase R, oligoadenylate synthases, adenosine deaminases acting on RNA, RNA interference systems, and other proteins containing dsRNA-binding domains and helicase domains. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1146/annurev-immunol-042718-041356DOI Listing
January 2019

Physical properties, ligand substitution reactions, and biological activity of Co(iii)-Schiff base complexes.

Dalton Trans 2019 Jan 23. Epub 2019 Jan 23.

Department of Chemistry and Chemical Biology, Cornell University, Ithaca, NY 14853, USA.

Four cobalt(iii) complexes of the general formula [Co(Schiff base)(L)2]+, where L is ammonia (NH3) or 3-fluorobenzylamine (3F-BnNH2), were synthesized. The complexes were characterized by NMR spectroscopy, mass spectrometry, and X-ray crystallography. Their electrochemical properties, ligand substitution mechanisms, and ligand exchange rates in aqueous buffer were investigated. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1039/c8dt04606aDOI Listing
January 2019
1 Read

Evaluation of anti-HSV-1 activity and toxicity of hydroethanolic extract of Tanacetum parthenium (L.) Sch.Bip. (Asteraceae).

Phytomedicine 2018 Aug 13;55:249-254. Epub 2018 Aug 13.

Department of Basic Health Sciences, State University of Maringá, Maringá, Paraná, Brazil. Electronic address:

Background: Herpes simplex type 1 (HSV-1) is widely distributed throughout the world's population. The virus spreads through direct contact with an infected individual. After primary infection, the virus remains in a latent state, and the recurrence of herpetic lesions is common. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.phymed.2018.06.040DOI Listing
August 2018
2 Reads

Usefulness of Adult Medaka Fish as a Model for the Evaluation of Alcoholic Fatty Liver.

Alcohol 2019 Jan 17. Epub 2019 Jan 17.

Center for Regenerative Medicine, Yamaguchi University School of Medicine, Minami Kogushi 1-1-1, Ube Yamaguchi 755-8505, Japan; Department of Gastroenterology and Hepatology, Yamaguchi University Graduate School of Medicine, Ube Yamaguchi 755-8505, Japan.

Alcohol has long been acknowledged to be one of the main causes of hepatic disorders. In recent years, with the advancements in antiviral therapies, the relative proportion alcoholic liver disease constitutes among liver diseases has increased, necessitating the establishment of a useful model for the elucidation of the mechanism of its development. In this study, we developed a model of alcoholic liver disease using medaka, a small-sized fish known for its usefulness as a model organism. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.alcohol.2019.01.005DOI Listing
January 2019
1 Read

Antiviral immunity in chronic lymphocytic leukemia measured by anti-rubella antibody.

Adv Clin Exp Med 2019 Jan 17. Epub 2019 Jan 17.

Department of Clinical Pharmacology, Wroclaw Medical University, Poland.

Background: Chronic lymphocytic leukemia (CLL), the most common form of adult leukemia in Caucasian populations, is characterized by a decrease in anti-infective immunity. Clinical evidence of antiviral immunity decrease is the reactivation of herpes virus in the form of skin lesions. In Europe, rubella infection is common and creates lifelong persistence of IgG antibodies. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.17219/acem/94164DOI Listing
January 2019
2 Reads

Anti-zika virus activity of polyoxometalates.

Antiviral Res 2019 Mar 14;163:29-33. Epub 2019 Jan 14.

Department of Clinical and Biological Sciences, Laboratory of Molecular Virology and Antiviral Research, University of Turin, S. Luigi Gonzaga Hospital, Orbassano Turin, Italy. Electronic address:

Zika virus (ZIKV) is an emerging infectious viral pathogen associated with severe fetal cerebral anomalies and the paralytic Guillain-Barrè syndrome in adults. It was the cause of a recent global health crisis following its entrance into a naïve population in the Americas. Nowadays, no vaccine or specific antiviral against ZIKV is available. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.antiviral.2019.01.005DOI Listing
March 2019
2 Reads

Evaluation on the antiviral activity of ribavirin against infectious hematopoietic necrosis virus in epithelioma papulosum cyprini cells.

Virus Res 2019 Jan 14;263:73-79. Epub 2019 Jan 14.

College of Animal Science and Technology, Northwest A&F University, Xinong Road 22nd, Yangling, Shaanxi, 712100, China. Electronic address:

Infectious hematopoietic necrosis virus (IHNV) causes high mortality in several economically important salmonid fishes, but there is no approved therapy up to now. To address the urgent need for therapeutics to combat IHNV infection, we investigate the anti-IHNV activities of 14 common antiviral agents using epithelioma papulosum cyprini (EPC) cells in this study. Among these agents, ribavirin shows the highest inhibition on IHNV replication, with an inhibitory percentage of 99. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.virusres.2019.01.008DOI Listing
January 2019
2 Reads

Baloxavir marboxil (Xofluza) for treatment of influenza.

Authors:

Med Lett Drugs Ther 2018 Dec;60(1561):193-196

View Article

Download full-text PDF

Source
December 2018

Virus-induced accumulation of intracellular bile acids activates the TGR5-β-arrestin-SRC axis to enable innate antiviral immunity.

Cell Res 2019 Jan 16. Epub 2019 Jan 16.

Department of Infectious Diseases, Zhongnan Hospital of Wuhan University, Wuhan, 430071, China.

The mechanisms on metabolic regulation of immune responses are still elusive. We show here that viral infection induces immediate-early NF-κB activation independent of viral nucleic acid-triggered signaling, which triggers a rapid transcriptional induction of bile acid (BA) transporter and rate-limiting biosynthesis enzymes as well as accumulation of intracellular BAs in divergent cell types. The accumulated intracellular BAs activate SRC kinase via the TGR5-GRK-β-arrestin axis, which mediates tyrosine phosphorylation of multiple antiviral signaling components including RIG-I, VISA/MAVS, MITA/STING, TBK1 and IRF3. Read More

View Article

Download full-text PDF

Source
http://www.nature.com/articles/s41422-018-0136-1
Publisher Site
http://dx.doi.org/10.1038/s41422-018-0136-1DOI Listing
January 2019
10 Reads
12.413 Impact Factor

Alpha-carboxynucleoside phosphonates: direct-acting inhibitors of viral DNA polymerases.

Future Med Chem 2019 Jan 16;11(2):137-154. Epub 2019 Jan 16.

Department of Chemistry, Analytical & Biological Chemistry Research Facility, Synthesis & Solid State Pharmaceutical Centre, University College, Cork, Ireland.

Acyclic nucleoside phosphonates represent a well-defined class of clinically used nucleoside analogs. All acyclic nucleoside phosphonates need intracellular phosphorylation before they can bind viral DNA polymerases. Recently, a novel class of alpha-carboxynucleoside phosphonates have been designed to mimic the natural 2'-deoxynucleotide 5'-triphosphate substrates of DNA polymerases. Read More

View Article

Download full-text PDF

Source
https://www.future-science.com/doi/10.4155/fmc-2018-0324
Publisher Site
http://dx.doi.org/10.4155/fmc-2018-0324DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6362432PMC
January 2019
4 Reads

Good and bad molecular fingerprints for human rhinovirus 3C protease inhibition: identification, validation, and application in designing of new inhibitors through Monte Carlo-based QSAR study.

J Biomol Struct Dyn 2019 Jan 16:1-12. Epub 2019 Jan 16.

a Laboratory of Drug Design and Discovery, Department of Pharmaceutical Sciences , Dr. Harisingh Gour University (A Central University) , Sagar , India.

HRV 3 C protease (HRV 3C) is an important target for common cold and upper respiratory tract infection. Keeping in view of the non-availability of drug for the treatment, newer computer-based modelling strategies should be applied to rationalize the process of antiviral drug discovery in order to decrease the valuable time and huge expenditure of the process. The present work demonstrates a structure wise optimization using Monte Carlo-based QSAR method that decomposes ligand compounds (in SMILES format) into several molecular fingerprints/descriptors. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1080/07391102.2019.1566093DOI Listing
January 2019
5 Reads
2.983 Impact Factor

Viral RNA-dependent RNA polymerase inhibitor 7-deaza-2'methyladenosine prevents death in a mouse model of West Nile virus infection.

Antimicrob Agents Chemother 2019 Jan 14. Epub 2019 Jan 14.

Department of Virology, Veterinary Research Institute, Hudcova 70, CZ-62100 Brno, Czech Republic

West Nile virus (WNV) is a medically important emerging arbovirus causing serious neuroinfections in humans against which no approved antiviral therapy is currently available. In this study, we demonstrate that 2'methyl- or 4'-azido-modified nucleosides are highly effective inhibitors of WNV replication, showing nanomolar or low micromolar anti-WNV activity and negligible cytotoxicity in cell culture. One representative of 2'-methylated nucleosides, 7-deaza-2'methyladenosine, significantly protected WNV-infected mice from disease progression and mortality. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1128/AAC.02093-18DOI Listing
January 2019
1 Read