journal
MENU ▼
Read by QxMD icon Read
search

Antiviral Chemistry & Chemotherapy

journal
https://www.readbyqxmd.com/read/29768937/cotton-rat-model-for-testing-vaccines-and-antivirals-against-respiratory-syncytial-virus
#1
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://www.readbyqxmd.com/read/29566538/frequent-cross-resistance-to-rilpivirine-among-subtype-c-hiv-1-from-first-line-antiretroviral-therapy-failures-in-south-africa
#2
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://www.readbyqxmd.com/read/29562753/nucleosides-for-the-treatment-of-respiratory-rna-virus-infections
#3
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://www.readbyqxmd.com/read/29546767/characterization-of-phenyl-pyrimidine-derivatives-that-inhibit-cytomegalovirus-immediate-early-gene-expression
#4
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://www.readbyqxmd.com/read/29534608/nucleoside-analogs-as-a-rich-source-of-antiviral-agents-active-against-arthropod-borne-flaviviruses
#5
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://www.readbyqxmd.com/read/29534607/addressing-the-selectivity-and-toxicity-of-antiviral-nucleosides
#6
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://www.readbyqxmd.com/read/29466861/flexibility-not-just-for-yoga-anymore
#7
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://www.readbyqxmd.com/read/29463095/current-and-future-use-of-nucleo-s-tide-prodrugs-in-the-treatment-of-hepatitis-c-virus-infection
#8
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://www.readbyqxmd.com/read/29436843/synthesis-and-substrate-properties-towards-hiv-1-reverse-transcriptase-of-new-diphosphate-analogues-of-9-2-phosphonomethoxy-ethyl-adenine
#9
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
https://www.readbyqxmd.com/read/29417826/indolylarylsulfones-a-fascinating-story-of-highly-potent-human-immunodeficiency-virus-type-1-non-nucleoside-reverse-transcriptase-inhibitors
#10
Valeria Famiglini, Romano Silvestri
Indolylarylsulfones are a potent class of human immunodeficiency virus type 1 non-nucleoside reverse transcriptase inhibitors. In this review, the structure activity relationship (SAR) studies to improve the profile of sulfone L-737,126 discovered by Merck AG have been analysed with focus on introduction of the 3',5'-dimethyl groups at the 3-phenylsulfonyl moiety, the 2-hydroxyethyl tail at the indole-2-carboxamide nitrogen, coupling of the carboxamide nitrogen with one or two glycinamide and alaninamide units, a fluorine atom at position 4 of the indole ring and correlation between configuration of the asymmetric centre and linker length...
January 2018: Antiviral Chemistry & Chemotherapy
https://www.readbyqxmd.com/read/29343083/polarized-macrophage-subsets-differentially-express-the-drug-efflux-transporters-mrp1-and-bcrp-resulting-in-altered-hiv-production
#11
Hui He, Merrion Buckley, Bernard Britton, Ying Mu, Kristin Warner, Santosh Kumar, Theodore J Cory
Introduction Macrophages play an important role in HIV, where they are a cellular reservoir. Macrophages are polarized into two phenotypes: pro-inflammatory M1 macrophages and anti-inflammatory M2 macrophages, which may have altered expression of drug efflux transporters, including BCRP and MRP1. These differences may result in subtherapeutic concentrations of antiretrovirals inside of macrophages and viral replication. Methods U937 and U1 cells were polarized to the M1 or M2 phenotype via IFN-γ and LPS, or IL-4, IL-13, and LPS...
January 2018: Antiviral Chemistry & Chemotherapy
https://www.readbyqxmd.com/read/29172646/3-7-dideazaneplanocin-synthesis-and-antiviral-analysis
#12
Xue-Qiang Yin, Stewart W Schneller
Objective To synthesize 3,7-dideazaneplanocin and evaluate its antiviral potential. Methods The target 3,7-dideazaneplanocin has been prepared in five steps from a readily available cyclopentenol. A thorough in vitro antiviral analysis was conducted versus both DNA and RNA viruses. Results A rational synthesis of 3,7-dideazaneplanocin was conceived and successfully pursued in such a way that it can be adapted to various analogs of 3,7-dideazaneplanocin. Using standard antiviral assays, no activity for 3,7-dideazaneplanocn was found...
December 2017: Antiviral Chemistry & Chemotherapy
https://www.readbyqxmd.com/read/29096526/establishment-of-an-antiviral-assay-system-and-identification-of-severe-fever-with-thrombocytopenia-syndrome-virus-inhibitors
#13
Masanori Baba, Masaaki Toyama, Norikazu Sakakibara, Mika Okamoto, Naomichi Arima, Masayuki Saijo
Aims Severe fever with thrombocytopenia syndrome (SFTS) is an emerging tick-borne infectious disease. SFTS is epidemic in Asia, and its fatality rate is around 30% in Japan. The causative virus severe fever with thrombocytopenia syndrome virus (SFTSV) is a phlebovirus of the family Phenuiviridae (the order Bunyavirales). Although effective treatments are required, there are no antiviral agents currently approved for clinical use. Ribavirin and favipiravir were examined for their anti-SFTSV activity and found to be selective inhibitors of SFTSV replication in vitro...
December 2017: Antiviral Chemistry & Chemotherapy
https://www.readbyqxmd.com/read/29096525/nucleoside-diphosphate-and-triphosphate-prodrugs-an-unsolvable-task
#14
REVIEW
Chris Meier
In this review, our recent advances in the development of nucleoside di- and nucleoside triphosphate prodrugs is summarized. Previously, we had developed a successful membrane-permeable pronucleotide system for the intracellular delivery of nucleoside monophosphates as well, the so-called cycloSal-approach. In contrast to that work in which the delivery is initiated by a chemically driven hydrolysis reaction, for the di- and triphosphate delivery, an enzymatic trigger mechanism involving (carboxy)esterases had to be used...
December 2017: Antiviral Chemistry & Chemotherapy
https://www.readbyqxmd.com/read/28893089/investigation-of-the-solvent-dependent-photolysis-of-a-nonnucleoside-reverse-transcriptase-inhibitor-antiviral-agent-efavirenz
#15
Maryam A Jordaan, Michael Shapi
This study sought to investigate the solvent-dependency on the photolysis of efavirenz to gain insight into the photoprocesses involved. The primary mechanisms were firstly the excited-state intramolecular proton transfer (i.e. phototautomerization), which generated the imidic acid phototautomer observed as [M-H]- quasimolecular ion at m/z 314.0070 in the high-performance liquid chromatography-electrospray ionization-time-of-flight mass spectrometry in the negative mode. Secondly, the photoinduced α-cleavage with the loss of a carbonyl group occurred (i...
December 2017: Antiviral Chemistry & Chemotherapy
https://www.readbyqxmd.com/read/28768435/cycluridine-a-novel-antiviral-effective-against-flaviviruses
#16
REVIEW
Angel S Galabov, Lucia Mukova, Yuriy P Abashev, Lilia Wassilewa, Petko Tzvetkov, Vassil Minkov, Igor F Barinskiy, Charles M Rice, Sergey Ouzounov, Dorotea Sidzhakova
This review describes the contemporary state of research for antivirals effective against flaviviruses, especially focusing on inhibitors of the pestivirus causative agent of bovine viral diarrhoea virus. We highlight cycluridine, an originally synthesized Mannich's base [a tetrahydro-2(1H)-pyrimidinones derivative], as a highly effective antiviral possessing a strong inhibitory effect on bovine viral diarrhoea virus replication. Cycluridine was active against replication of a wide variety of bovine viral diarrhoea virus strains in cell cultures...
August 2017: Antiviral Chemistry & Chemotherapy
https://www.readbyqxmd.com/read/28768434/metabolic-reprogramming-during-hepatitis-b-disease-progression-offers-novel-diagnostic-and-therapeutic-opportunities
#17
REVIEW
Jesse Jr Masson, Hugh Ww Billings, Clovis S Palmer
Metabolic remodeling occurs in immune cells during an infection. Host cells must upregulate energy production for growth, proliferation, and effector functions to limit the damage imposed by pathogens. One example, the hepatitis B virus, induces hepatic injury in human hepatocytes through dysregulation of aerobic glycolysis and lipid metabolism. Increased glycolytic metabolism mediated by elevated expression of Glut1, glucose influx, and lactate secretion is associated with this Warburg phenotype, a classic metabolic signature also observed in cancer cells...
August 2017: Antiviral Chemistry & Chemotherapy
https://www.readbyqxmd.com/read/28768433/editorial
#18
Andrea Brancale
No abstract text is available yet for this article.
August 2017: Antiviral Chemistry & Chemotherapy
https://www.readbyqxmd.com/read/28737040/potential-of-small-molecule-fungal-metabolites-in-antiviral-chemotherapy
#19
REVIEW
Biswajit G Roy
Various viral diseases, such as acquired immunodeficiency syndrome, influenza, and hepatitis, have emerged as leading causes of human death worldwide. Scientific endeavor since invention of DNA-dependent RNA polymerase of pox virus in 1967 resulted in better understanding of virus replication and development of various novel therapeutic strategies. Despite considerable advancement in every facet of drug discovery process, development of commercially viable, safe, and effective drugs for these viruses still remains a big challenge...
August 2017: Antiviral Chemistry & Chemotherapy
https://www.readbyqxmd.com/read/28417642/equilibrative-nucleoside-transporter-1-expression-in-primary-human-hepatocytes-is-highly-variable-and-determines-uptake-of-ribavirin
#20
Kanwal Baloch, Liqiong Chen, Ameer A Memon, Laura Dexter, William Irving, Mohammad Ilyas, Brian J Thomson
Aims Ribavirin is a nucleoside analogue and remains a necessary component of both interferon-based and directly acting anti-viral regimens for the treatment of hepatitis C virus infection. The achievable concentration of ribavirin within hepatocytes is likely to be an important determinant of therapeutic outcome. In vitro expression levels of equilibrative nucleoside transporter 1 (ENT1) has been shown to be a predictor of treatment response in patients receiving nucleoside-based chemotherapeutic agents. We therefore investigated whether a similar relationship existed between ENT1 expression and ribavirin uptake in freshly isolated primary hepatocytes...
April 2017: Antiviral Chemistry & Chemotherapy
journal
journal
30471
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"