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Antiviral Chemistry & Chemotherapy

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https://read.qxmd.com/read/30788976/synthesis-and-anti-human-immunodeficiency-virus-activity-of-substituted-o-o-difluorophenyl-linked-pyrimidines-as-potent-non-nucleoside-reverse-transcriptase-inhibitors
#1
Lucie Čechová, Milan Dejmek, Ondřej Baszczyňski, David Šaman, Liping Gao, Eric Hu, George Stepan, Petr Jansa, Zlatko Janeba, Petr Šimon
With the worldwide number of human immunodeficiency virus positive patients stagnant and the increasing emergence of viral strains resistant to current treatment, the development of novel anti-human immunodeficiency virus drug candidates is a perpetual quest of medicinal chemists. Herein, we report a novel group of diarylpyrimidines, non-nucleoside reverse transcriptase inhibitors, which represents an important class of current anti-human immunodeficiency virus therapy. Series of diarylpyrimidines containing o, o-difluorophenyl (A-arm), 4-cyanophenylamino (B-arm), and a small substituent (e...
January 2019: Antiviral Chemistry & Chemotherapy
https://read.qxmd.com/read/30776910/mozobil%C3%A2-plerixafor-amd3100-10-years-after-its-approval-by-the-us-food-and-drug-administration
#2
Erik De Clercq
AMD3100 (plerixafor, Mozobil®) was first identified as an anti-HIV agent specifically active against the T4-lymphotropic HIV strains, as it selectively blocked the CXCR4 receptor. Through interference with the interaction of CXCR4 with its natural ligand, SDF-1 (also named CXCL12), it also mobilized the CD34+ stem cells from the bone marrow into the peripheral blood stream. In December 2008, AMD3100 was formally approved by the US FDA for autologous transplantation in patients with Non-Hodgkin's Lymphoma or multiple myeloma...
January 2019: Antiviral Chemistry & Chemotherapy
https://read.qxmd.com/read/30759993/a-medium-throughput-screen-for-inhibitors-of-human-metapneumovirus
#3
Jennifer C Becker, Sharon J Tollefson, David Weaver, John V Williams
Human metapneumovirus, a paramyxovirus discovered in 2001, is a major cause of lower respiratory infection in adults and children worldwide. There are no licensed vaccines or drugs for human metapneumovirus. We developed a fluorescent, cell-based medium-throughput screening assay for human metapneumovirus that captures inhibitors of all stages of the viral lifecycle except budding of progeny virus particles from the cell membrane. We optimized and validated the assay and performed a successful medium-throughput screening...
January 2019: Antiviral Chemistry & Chemotherapy
https://read.qxmd.com/read/30497281/xanthine-based-acyclic-nucleoside-phosphonates-with-potent-antiviral-activity-against-varicella-zoster-virus-and-human-cytomegalovirus
#4
Ondřej Baszczyňski, Martin Maxmilian Kaiser, Michal Česnek, Petra Břehová, Petr Jansa, Eliška Procházková, Martin Dračínský, Robert Snoeck, Graciela Andrei, Zlatko Janeba
While noncanonic xanthine nucleotides XMP/dXMP play an important role in balancing and maintaining intracellular purine nucleotide pool as well as in potential mutagenesis, surprisingly, acyclic nucleoside phosphonates bearing a xanthine nucleobase have not been studied so far for their antiviral properties. Herein, we report the synthesis of a series of xanthine-based acyclic nucleoside phosphonates and evaluation of their activity against a wide range of DNA and RNA viruses. Two acyclic nucleoside phosphonates within the series, namely 9-[2-(phosphonomethoxy)ethyl]xanthine (PMEX) and 9-[3-hydroxy-2-(phosphonomethoxy)propyl]xanthine (HPMPX), were shown to possess activity against several human herpesviruses...
January 2018: Antiviral Chemistry & Chemotherapy
https://read.qxmd.com/read/30466301/activity-of-enisamium-an-isonicotinic-acid-derivative-against-influenza-viruses-in-differentiated-normal-human-bronchial-epithelial-cells
#5
David Boltz, Xinjian Peng, Miguel Muzzio, Pradyot Dash, Paul G Thomas, Victor Margitich
AIMS: New therapeutics for the control of influenza virus infections are needed to alleviate the burden caused by seasonal epidemics and occasional pandemics, and to overcome the potential risk of drug-resistance emergence. Enisamium iodide (Amizon®, Farmak) is currently approved for clinical use for the treatment of influenza in 11 countries which includes Ukraine, Russia, Belarus, Kazakhstan, and Uzbekistan. However, experimental evidence of the antiviral activity of enisamium has not been reported...
January 2018: Antiviral Chemistry & Chemotherapy
https://read.qxmd.com/read/30449131/cyclophilin-a-as-a-target-in-the-treatment-of-cytomegalovirus-infections
#6
Ashwaq A Abdullah, Rasedee Abdullah, Zeenathul A Nazariah, Krishnan N Balakrishnan, Faez Firdaus J Abdullah, Jamilu A Bala, Mohd-Azmi Mohd-Lila
BACKGROUND: Viruses are obligate parasites that depend on the cellular machinery of the host to regenerate and manufacture their proteins. Most antiviral drugs on the market today target viral proteins. However, the more recent strategies involve targeting the host cell proteins or pathways that mediate viral replication. This new approach would be effective for most viruses while minimizing drug resistance and toxicity. METHODS: Cytomegalovirus replication, latency, and immune response are mediated by the intermediate early protein 2, the main protein that determines the effectiveness of drugs in cytomegalovirus inhibition...
January 2018: Antiviral Chemistry & Chemotherapy
https://read.qxmd.com/read/30354193/the-effectiveness-of-antiviral-agents-with-broad-spectrum-activity-against-chikungunya-virus-varies-between-host-cell-lines
#7
Evelyn J Franco, Jaime L Rodriquez, Justin J Pomeroy, Kaley C Hanrahan, Ashley N Brown
Chikungunya virus (CHIKV) is a mosquito-borne virus that has recently emerged in the Western Hemisphere. Approved antiviral therapies or vaccines for the treatment or prevention of CHIKV infections are not available. This study aims to evaluate the antiviral activity of commercially available broad-spectrum antivirals against CHIKV. Due to host cell-specific variability in uptake and intracellular processing of drug, we evaluated the antiviral effects of each agent in three cell lines. Antiviral activities of ribavirin (RBV), interferon-alfa (IFN-α) and favipiravir (FAV) were assessed in CHIKV-infected Vero, HUH-7, and A549 cells...
January 2018: Antiviral Chemistry & Chemotherapy
https://read.qxmd.com/read/30016878/corrigendum
#8
(no author information available yet)
Galabov AS, Mukova L, Abashev YP, Wassilewa L, Tzvetkov P, Minkov V, Barinskiy IF, Ouzounov S, Sidzhakova D. Cycluridine: A novel antiviral effective against flaviviruses. ‎ Antivir. Chem. Chemother 2017; 25: 58-67. DOI: 10.1177/2040206617723442 The authors acknowledge that Charles M Rice did not co-author or contribute to this article and was erroneously listed as co-author. The correct authorship is indicated above. The article has been corrected.
January 2018: Antiviral Chemistry & Chemotherapy
https://read.qxmd.com/read/29954186/meeting-report-30th-international-conference-on-antiviral-research-in-atlanta-ga-usa
#9
R Anthony Vere Hodge
The 30th International Conference on Antiviral Research was held in Atlanta, GA, USA, from 21 to 25 May 2017. Each year, the International Society for Antiviral Research (ISAR) presents three major awards, this year to Mike Sofia (Elion award), David Chu (Holý award) and Maaike Everts (Prusoff award). Also this year, the inaugural ISAR Women in Science award lecture was presented by Priscilla Yang. For several years, International Conference on Antiviral Research (ICAR) has included at least one Keynote lecture, this year there were four...
January 2018: Antiviral Chemistry & Chemotherapy
https://read.qxmd.com/read/29890841/advances-in-antiviral-nucleoside-analogues-and-their-prodrugs
#10
Katherine Seley-Radtke, Jerome Deval
No abstract text is available yet for this article.
January 2018: Antiviral Chemistry & Chemotherapy
https://read.qxmd.com/read/29792071/phosphoramidates-and-phosphonamidates-protides-with-antiviral-activity
#11
Magdalena Slusarczyk, Michaela Serpi, Fabrizio Pertusati
Following the first report on the nucleoside phosphoramidate (ProTide) prodrug approach in 1990 by Chris McGuigan, the extensive investigation of ProTide technology has begun in many laboratories. Designed with aim to overcome limitations and the key resistance mechanisms associated with nucleoside analogues used in the clinic (poor cellular uptake, poor conversion to the 5'-monophosphate form), the ProTide approach has been successfully applied to a vast number of nucleoside analogues with antiviral and anticancer activity...
January 2018: Antiviral Chemistry & Chemotherapy
https://read.qxmd.com/read/29768937/cotton-rat-model-for-testing-vaccines-and-antivirals-against-respiratory-syncytial-virus
#12
M S Boukhvalova, K C Yim, Jcg Blanco
Respiratory syncytial virus is the leading cause of pneumonia and bronchiolitis in infants and is a serious health risk for elderly and immunocompromised individuals. No vaccine has yet been approved to prevent respiratory syncytial virus infection and the only available treatment is immunoprophylaxis of severe respiratory syncytial virus disease in high-risk infants with Palivizumab (Synagis® ). The development of respiratory syncytial virus vaccine has been hampered by the phenomenon of enhanced respiratory syncytial virus disease observed during trials of a formalin-inactivated respiratory syncytial virus in 1960s...
January 2018: Antiviral Chemistry & Chemotherapy
https://read.qxmd.com/read/29566538/frequent-cross-resistance-to-rilpivirine-among-subtype-c-hiv-1-from-first-line-antiretroviral-therapy-failures-in-south-africa
#13
Kerri J Penrose, Chanson J Brumme, Maritsa Scoulos-Hanson, Kristen Hamanishi, Kelley Gordon, Raquel V Viana, Carole L Wallis, P Richard Harrigan, John W Mellors, Urvi M Parikh
Background Rilpivirine (TMC278LA) is a promising drug for pre-exposure prophylaxis of HIV-1 because of its sub-nanomolar potency and long-acting formulation; however, increasing transmission of non-nucleoside reverse transcriptase inhibitor-resistant HIV-1 with potential cross-resistance to rilpivirine could reduce its preventive efficacy. This study investigated rilpivirine cross-resistance among recombinant subtype C HIV-1 derived from 100 individuals failing on first-line non-nucleoside reverse transcriptase inhibitor-containing antiretroviral therapy in South Africa whose samples were sent for routine HIV-1 drug resistance testing to Lancet Laboratories (Johannesburg, South Africa)...
January 2018: Antiviral Chemistry & Chemotherapy
https://read.qxmd.com/read/29562753/nucleosides-for-the-treatment-of-respiratory-rna-virus-infections
#14
Paul C Jordan, Sarah K Stevens, Jerome Deval
Influenza virus, respiratory syncytial virus, human metapneumovirus, parainfluenza virus, coronaviruses, and rhinoviruses are among the most common viruses causing mild seasonal colds. These RNA viruses can also cause lower respiratory tract infections leading to bronchiolitis and pneumonia. Young children, the elderly, and patients with compromised cardiac, pulmonary, or immune systems are at greatest risk for serious disease associated with these RNA virus respiratory infections. In addition, swine and avian influenza viruses, together with severe acute respiratory syndrome-associated and Middle Eastern respiratory syndrome coronaviruses, represent significant pandemic threats to the general population...
January 2018: Antiviral Chemistry & Chemotherapy
https://read.qxmd.com/read/29546767/characterization-of-phenyl-pyrimidine-derivatives-that-inhibit-cytomegalovirus-immediate-early-gene-expression
#15
Koh-Hei Yamada, Ryuichi Majima, Toyofumi Yamaguchi, Naoki Inoue
Background Previously, we established a reporter cell line for human cytomegalovirus and screened anti-human cytomegalovirus compounds using the cell line. In this study, we characterized one of the identified compounds, 2,4-diamino-6-(4-methoxyphenyl)pyrimidine (coded as 35C10). Methods 50% Effective concentrations (EC50s) and 50% cytotoxic concentrations (CC50s) of 35C10 and its derivatives in human fibroblasts were determined by X-gal staining of the cells infected with human cytomegalovirus Towne strain expressing β-galactosidase...
January 2018: Antiviral Chemistry & Chemotherapy
https://read.qxmd.com/read/29534608/nucleoside-analogs-as-a-rich-source-of-antiviral-agents-active-against-arthropod-borne-flaviviruses
#16
Luděk Eyer, Radim Nencka, Erik de Clercq, Katherine Seley-Radtke, Daniel Růžek
Nucleoside analogs represent the largest class of small molecule-based antivirals, which currently form the backbone of chemotherapy of chronic infections caused by HIV, hepatitis B or C viruses, and herpes viruses. High antiviral potency and favorable pharmacokinetics parameters make some nucleoside analogs suitable also for the treatment of acute infections caused by other medically important RNA and DNA viruses. This review summarizes available information on antiviral research of nucleoside analogs against arthropod-borne members of the genus Flavivirus within the family Flaviviridae, being primarily focused on description of nucleoside inhibitors of flaviviral RNA-dependent RNA polymerase, methyltransferase, and helicase/NTPase...
January 2018: Antiviral Chemistry & Chemotherapy
https://read.qxmd.com/read/29534607/addressing-the-selectivity-and-toxicity-of-antiviral-nucleosides
#17
Joy Y Feng
Nucleoside and nucleotide analogs have played significant roles in antiviral therapies and are valued for their impressive potency and high barrier to resistance. They have been approved for treatment of herpes simplex virus-1, HIV, HBV, HCV, and influenza, and new drugs are being developed for the treatment of RSV, Ebola, coronavirus MERS, and other emerging viruses. However, this class of compounds has also experienced a high attrition rate in clinical trials due to toxicity. In this review, we discuss the utility of different biochemical and cell-based assays and provide recommendations for assessing toxicity liability before entering animal toxicity studies...
January 2018: Antiviral Chemistry & Chemotherapy
https://read.qxmd.com/read/29466861/flexibility-not-just-for-yoga-anymore
#18
Katherine Seley-Radtke
Over the past few years, nucleosides have maintained a prominent role as one of the cornerstones of antiviral and anticancer therapeutics, and many approaches to nucleoside drug design have been pursued. One such approach involves flexibility in the sugar moiety of nucleosides, for example, in the highly successful anti-HIV and HBV drug tenofovir. In contrast, introduction of flexibility to the nucleobase scaffold has only more recently gained significance with the invention of our fleximers. The history, development, and some biological relevance for this innovative class of nucleosides are detailed herein...
January 2018: Antiviral Chemistry & Chemotherapy
https://read.qxmd.com/read/29463095/current-and-future-use-of-nucleo-s-tide-prodrugs-in-the-treatment-of-hepatitis-c-virus-infection
#19
Cyril B Dousson
This review describes the current state of discovery of past most important nucleoside and nucleotide prodrugs in the treatment of hepatitis C virus infection as well as future potential drugs currently in discovery or clinical evaluation. I highlight first generation landmark prodrug compounds which have been the foundations of incremental improvements toward the discovery and approval milestone of Sofosbuvir. Sofosbuvir is the first nucleotide prodrug marketed for hepatitis C virus treatment and the backbone of current combination therapies...
January 2018: Antiviral Chemistry & Chemotherapy
https://read.qxmd.com/read/29436843/synthesis-and-substrate-properties-towards-hiv-1-reverse-transcriptase-of-new-diphosphate-analogues-of-9-2-phosphonomethoxy-ethyl-adenine
#20
Wolfgang Hg Laux, Stéphane Priet, Karine Alvarez, Suzanne Peyrottes, Christian Périgaud
Background The replacement of β,γ-pyrophosphate by β,γ-phosphonate moieties within the triphosphate chain of 5'-triphosphate nucleoside analogues was previously studied for various antiviral nucleoside analogues such as AZT and 2',3'-dideoxynucleosides. Thus, it has been shown that these chemical modifications could preserve, in some cases, the terminating substrate properties of the triphosphate analogue for HIV-RT. Herein, we aimed to study such 5'-triphosphate mimics based on the scaffold of the well-known antiviral agent 9-[(2-phosphonomethoxy)ethyl]adenine (PMEA, Adefovir)...
January 2018: Antiviral Chemistry & Chemotherapy
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