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Antiviral Chemistry & Chemotherapy

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
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
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
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
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...
November 3, 2017: Antiviral Chemistry & Chemotherapy
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...
November 3, 2017: Antiviral Chemistry & Chemotherapy
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
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
Andrea Brancale
No abstract text is available yet for this article.
August 2017: Antiviral Chemistry & Chemotherapy
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
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
Andrea Brancale
No abstract text is available yet for this article.
April 2017: Antiviral Chemistry & Chemotherapy
Donald F Smee, Ashley Dagley, E B Tarbet
L-N(G)-monomethyl-arginine (L-NMMA) is an experimental compound that suppresses nitric oxide production in animals. The compound was combined with oseltamivir to treat lethal influenza A/California/04/2009 (H1N1) pandemic virus infections in mice. Treatments were given twice a day for five days starting 4 h (oseltamivir, by oral gavage) or three days (L-NMMA, by intraperitoneal route; corresponding to the time previously reported for nitric oxide induction in the animals) after infection. Low doses of oseltamivir were used in order to demonstrate synergy or antagonism...
April 2017: Antiviral Chemistry & Chemotherapy
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...
January 1, 2017: Antiviral Chemistry & Chemotherapy
Marcella Bassetto, Salvatore Ferla, Pieter Leyssen, Johan Neyts, Mark M Yerukhimovich, David N Frick, Rachel O'Donnell, Andrea Brancale
BACKGROUND: Despite the great progress made in the last 10 years, alternative strategies might help improving definitive treatment options against hepatitis C virus infection. METHODS: With the aim of identifying novel inhibitors of the hepatitis C virus-1b replication targeting the viral NS3 helicase, the structures of previously reported symmetrical inhibitors of this enzyme were rationally modified, and according to docking-based studies, four novel scaffolds were selected for synthesis and evaluation in the hepatitis C virus-1b subgenomic replicon assay...
November 4, 2016: Antiviral Chemistry & Chemotherapy
Adelina Stoyanova, Ivanka Nikolova, Gerhard Pürstinger, Georgi Dobrikov, Vladimir Dimitrov, Stefan Philipov, Angel S Galabov
BACKGROUND: Chemotherapy is an important tool for controlling enterovirus infections, but clinically effective anti-enterovirus drugs do not currently exist, mainly due to the development of drug resistance. We investigated the combination effects of enterovirus replication inhibitors in order to limit this process. In previous studies, we showed the efficacy of consecutive alternating administration of the triple combinations disoxaril/guanidine/oxoglaucine and pleconaril/guanidine/oxoglaucine against coxsackievirus B1 infection in newborn mice...
November 4, 2016: Antiviral Chemistry & Chemotherapy
Sutthiwan Thammawat, Tania A Sadlon, Penelope Adamson, David L Gordon
Human metapneumovirus is an emerging cause of lower respiratory disease in infants, young children, and immunocompromised adults. We have previously demonstrated that human metapneumovirus infection is mediated by interaction of human metapneumovirus attachment (G) and/or fusion (F) proteins with cellular glycosaminoglycans. We report here the activity of an investigational sialidase fusion protein, DAS181, on human metapneumovirus infection of Hep-2 cells. These results suggest that human metapneumovirus infection may involve sialic acids, providing a new therapeutic strategy for human metapneumovirus for which there is currently no available treatment...
September 12, 2016: Antiviral Chemistry & Chemotherapy
Wataru Ito, Masaaki Toyama, Mika Okamoto, Masanori Ikeda, Koichi Watashi, Takaji Wakita, Yuichi Hashimoto, Masanori Baba
BACKGROUND: The novel phenanthridinone derivative HA-719 has recently been identified as a highly potent and selective inhibitor of hepatitis C virus replication. To elucidate its mechanism of inhibition, we have isolated and analyzed a clone of hepatitis C virus replicon cells resistant to HA-719. METHODS: To isolate HA-719-resistant replicon cells, Huh-7 cells containing subgenomic hepatitis C virus replicons (genotype 1b) with a luciferase reporter (LucNeo#2) were cultured in the presence of G418 and escalating concentrations of HA-719...
August 8, 2016: Antiviral Chemistry & Chemotherapy
Milagros Montiel, Ernesto Bonilla, Nereida Valero, Jesús Mosquera, Luz M Espina, Yasmir Quiroz, Melchor Álvarez-Mon
BACKGROUND: Pro-inflammatory and oxidative events during brain Venezuelan equine encephalitis virus infection could lead to apoptosis and induce anti-inflammatory responses (increased expression of CD200). The aim of this study was to determine the effect of melatonin on brain apoptosis, oxidative stress, and CD200 molecule in mice and neuroblastoma cultures infected by Venezuelan equine encephalitis virus. METHODS: Mice were infected with 10 median lethal doses (LD50) of Venezuelan equine encephalitis virus, treated with melatonin (500 µg/kg bw; three days before infection and during all experimental time) and sacrificed on days 1, 3, and 5 postinfection...
August 2015: Antiviral Chemistry & Chemotherapy
Angel S Galabov, Milka Mileva, Lora Simeonova, Galina Gegova
BACKGROUND: Influenza is a highly contagious viral infection of the respiratory system. To attack two processes involved in flu pathogenesis-viral replication in the infected body and oxidative damages, we studied the combination effect of neuraminidase inhibitor oseltamivir and antioxidant α-tocopherol in experimental model of influenza. METHODS: After inoculation of albino mice with 10 MLD50 (50% mouse lethal dose) of influenza virus A/Aichi/2/68 (H3N2), oseltamivir was applied orally at three doses, 2...
August 2015: Antiviral Chemistry & Chemotherapy
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