Abstract:
:On the basis of three different models (namely: ddU, AZT and PMEA), mononucleotide phosphotriester derivatives were designed to be able to liberate the corresponding monophosphate (or phosphonate) inside the cell through a reductase-mediated activation process. It was demonstrated that the use of bis[S-(2-hydroxyethylsulfidyl)-2-thioethyl] esters of ddUMP (11), AZTMP (12) and PMEA (17) resulted in intracellular delivery of the parent monophosphate (or phosphonate). This point was corroborated by observation of an anti-HIV effect of, 11 in various cell lines, for 12 in CEM TK- cells and by the enhanced activity observed for 17. Furthermore, the reported decomposition data in cell extracts fully confirm the validity of this approach and show unambiguously the potential for intracellular reductase-mediated activation of the starting drug.
journal_name
Antiviral Resjournal_title
Antiviral researchauthors
Puech F,Gosselin G,Lefebvre I,Pompon A,Aubertin AM,Kirn A,Imbach JLdoi
10.1016/0166-3542(93)90093-xsubject
Has Abstractpub_date
1993-10-01 00:00:00pages
155-74issue
2-3eissn
0166-3542issn
1872-9096pii
0166-3542(93)90093-Xjournal_volume
22pub_type
杂志文章abstract::A new adamantane derivative N,N'-bis (ethylene)P(1-adamantyl)-phosphonis diamide, was found to inhibit Rous sarcoma virus replication in much the same manner as reported for the parent compound, 1-adamantanamine hydrochloride. ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(81)90017-6
更新日期:1981-11-01 00:00:00
abstract::The bicyclams represent a new class of highly potent and selective HIV inhibitors. Time-of-addition experiments have previously shown that these compounds interfere with an early event in the viral replicative cycle. Additional experiments have now been carried out in order to investigate in more detail the mechanism ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(95)00837-3
更新日期:1996-03-01 00:00:00
abstract::Human parainfluenza virus type 3 (HPIV3) is an important respiratory tract pathogen of infants and children. There are no vaccines or antivirals currently approved for prevention or treatment of HPIV3 infection. Towards developing an antiviral therapy to combat HPIV3 infection, we have established a green fluorescent ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2007.09.001
更新日期:2008-02-01 00:00:00
abstract::Current therapies for chronic hepatitis B virus infection (CHB) - nucleos(t)ide analogue reverse transcriptase inhibitors and interferons - result in low rates of functional cure defined as sustained off-therapy seroclearance of hepatitis B surface antigen (HBsAg). One likely reason is the inability of these therapies...
journal_title:Antiviral research
pub_type: 杂志文章,评审
doi:10.1016/j.antiviral.2015.06.019
更新日期:2015-09-01 00:00:00
abstract::A series of four mannose(Man)-, three N-acetylglucosamine (GlcNAc)n-, ten N-acetylgalactosamine/galactose(GalNAc/Gal)-, one 5-acetylneuraminic acid (alpha-2,3-Gal/GalNAc)- and one 5-acetylneuroaminic acid(alpha-2,6-Gal/Gal-NAc)-specific plant agglutinins were evaluated for their antiviral activity in vitro. the mannos...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(92)90038-7
更新日期:1992-06-01 00:00:00
abstract::Preventive intraperitoneal trehalose dimycolate (TDM) treatment of mice, inoculated with encephalomyocarditis (EMC) virus by the same route, caused restriction of virus growth in the peritoneum, which was correlated to IFN production in peritoneal fluids prior to infection. Peritoneal macrophages from TDM-treated mice...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(95)00047-p
更新日期:1995-10-01 00:00:00
abstract::Itraconazole (ITZ) is a well-known, FDA-approved antifungal drug that is also in clinical trials for its anticancer activity. ITZ exerts its anticancer activity through several disparate targets and pathways. ITZ inhibits angiogenesis by hampering the functioning of the vascular endothelial growth receptor 2 (VEGFR2) ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2018.05.010
更新日期:2018-08-01 00:00:00
abstract::Three SAH hydrolase inhibitors, (RS)-3-adenin-9-yl-2-hydroxypropanoic acid (isobutyl ester) [(RS)-AHPA]; (RS)-9-(2,3-dihydroxypropyl)adenine [(RS)-DHPA] and the carbocyclic analog of 3-deazaadenosine (C-c3Ado) were evaluated for their inhibitory activity against tobacco mosaic virus (TMV) and potato virus X (PVX). Usi...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(90)90067-h
更新日期:1990-05-01 00:00:00
abstract::Although highly active anti-retroviral therapy (HAART) is successful in the treatment of HIV infection, problems with toxicity, drug-resistant variants, and therapeutic failures have compromised the long-term utility of existing combination regimens. Mismatched double-stranded RNA (polyI-polyC(12)U) is an immune modul...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/s0166-3542(01)00150-4
更新日期:2001-09-01 00:00:00
abstract::The effects of HIV-1 protease inhibitors on proteolytic processing and infectivity of virions produced from lymphocytes chronically infected with the virus were studied. Protease inhibition was detected by the accumulation of the polyprotein precursors Pr55gag and Pr160gag-pol and their cleavage intermediates. Immunob...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/s0166-3542(99)00074-1
更新日期:2000-01-01 00:00:00
abstract::Cats infected with molecularly cloned FeLV-FAIDS develop an immunodeficiency syndrome characterized by persistent antigenemia, decline in circulating CD4+ T lymphocytes, and impaired T-cell-dependent immune responses and opportunistic infection. We evaluated the capacity of PMEA to inhibit the replication of FeLV-FAID...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(91)90060-5
更新日期:1991-07-01 00:00:00
abstract:OBJECTIVE:We sought to investigate the differences in monocyte immune responses to the dengue virus (DENV) in those who previously had either severe disease (past SD) or non-severe dengue (past NSD) following a secondary dengue infection. METHOD:Monocytes from healthy individuals who had either past SD (n = 6) or past...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2019.104554
更新日期:2019-09-01 00:00:00
abstract::Prevention of HIV infection and unintended pregnancies are public health priorities. In sub-Saharan Africa, where HIV prevalence is highest, depot medroxyprogesterone acetate (DMPA) is widely used as contraception. Therefore, understanding potential interactions between DMPA and antiretrovirals is critical. Here, we u...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2020.105001
更新日期:2020-12-29 00:00:00
abstract::In Western countries, chronic hepatitis C virus (HCV)-infection mostly affects former and active substance users. The effect of active substance use on interferon (IFN)-responsiveness and therapy efficacy is not well understood. In this study, we compared natural killer (NK) cell activity and function in healthy contr...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2012.12.025
更新日期:2013-03-01 00:00:00
abstract::More than 50% of a group of healthy homosexuals in Israel were found to have an activated interferon (IFN) system as evidenced by markedly elevated blood IFN levels, increased in vitro production of IFN by unstimulated peripheral blood mononuclear cells and HuIFN-alpha and HuIFN-gamma production by appropriately stimu...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(85)90027-0
更新日期:1985-08-01 00:00:00
abstract::During studies of the antiviral activity of chalcone Ro-09-0410 on human rhinovirus type 9 (RV9) chalcone-resistant strains of RV9 were isolated and appeared with a frequency of about 10(-5) in chalcone sensitive stock. Chalcone-dependent viruses were found after further passage. Some characteristics of the resistant ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(87)90085-4
更新日期:1987-08-01 00:00:00
abstract::Despite an urgent medical need, a broadly effective anti-viral therapy for the treatment of infections with hepatitis C viruses (HCVs) has yet to be developed. One of the approaches to anti-HCV drug discovery is the design and development of specific small molecule drugs to inhibit the proteolytic processing of the HC...
journal_title:Antiviral research
pub_type: 杂志文章,评审
doi:
更新日期:1999-02-01 00:00:00
abstract::We report the design, synthesis, and biological evaluation of a class of 1H-pyrido[2,1-b][1,3]benzothiazol-1-ones originated from compound 1, previously identified as anti-flavivirus agent. Some of the new compounds showed activity in low μM range with reasonable selectivity against Dengue 2, Yellow fever (Bolivia str...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2019.03.004
更新日期:2019-07-01 00:00:00
abstract::This study aimed to investigate anti-HBV effect and major active compounds of Su-duxing, a medicine extracted from Chinese herbs. HBV-replicating cell lines HepG2.2.15 (wild-type) and HepG2.A64 (entecavir-resistant) were used for in vitro test. C57BL/6 mice infected by adeno-associated virus carrying 1.3 mer wild-type...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2018.04.017
更新日期:2018-07-01 00:00:00
abstract::Dolutegravir (S/GSK1349572) is a second-generation HIV-1 integrase inhibitor (INI) in advanced clinical development. It has shown good antiviral activity in most patients with prior raltegravir failure, although changes at the integrase codon 148, particularly when combined with other mutations, confer reduced suscept...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2011.03.178
更新日期:2011-06-01 00:00:00
abstract::Twenty-four patients with chronic non-A non-B hepatitis were randomly assigned to receive either human fibroblast interferon (HuIFN-beta) at doses of 1 or 3 million international units (MIU) per day for 4 or 12 weeks (12 patients) or to receive no therapy (12 patients), and were then compared with 5 patients with chro...
journal_title:Antiviral research
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1016/0166-3542(89)90048-x
更新日期:1989-10-01 00:00:00
abstract::RNase L is a cellular endoribonuclease that is activated by 2',5'-linked oligoadenylates (2-5A), which are unique and specific ligands synthesized by a family of interferon-inducible, dsRNA-activated enzymes named oligoadenylate synthetases. In the typical antiviral pathway, activated RNase L degrades viral and cellul...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2014.01.021
更新日期:2014-04-01 00:00:00
abstract::Sixteen herpes simplex virus type 1 (HSV-1) and four type 2 (HSV-2) isolates resistant to acyclovir (ACV) were characterized retrospectively for drug resistance. Phenotypic testing was performed by means of tetrazolium reduction assay and genotypic analysis was carried out by sequencing of thymidine kinase (TK) and DN...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2010.03.002
更新日期:2010-06-01 00:00:00
abstract::There are no drugs approved specifically to treat disseminated adenovirus (Ad) infections in humans. Cidofovir is active against Ad in cell culture, and it is used frequently in the clinic with disseminated infection in pediatric transplant patients; however, controlled clinical studies have not been conducted to prov...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2014.10.005
更新日期:2014-12-01 00:00:00
abstract::The chemically modified DNA, apurinic acid (APA), is cytotoxic for human lymphocytes at concentrations above 100 micrograms/ml. At low concentrations (0.05-1 micrograms/ml) APA acts as an inducer interferon gamma (IFN-gamma) in lymphocytes in vitro; the maximum interferon titer of 50 units/ml was reached at 0.4 microg...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(88)90003-4
更新日期:1988-04-01 00:00:00
abstract::Many flaviviruses, such as Zika virus (ZIKV), Dengue virus (DENV1-4) and yellow fever virus (YFV), are significant human pathogens. Infection with ZIKV, an emerging mosquito-borne flavivirus, is associated with increased risk of microcephaly in newborns and Guillain-Barré syndrome and other complications in adults. Cu...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2017.12.018
更新日期:2018-02-01 00:00:00
abstract::Pyrosequencing has been successfully used to monitor resistance in influenza A viruses to the first class of anti-influenza drugs, M2 blockers (adamantanes). In contrast to M2 blockers, resistance to neuraminidase (NA) inhibitors (NAIs) is subtype- and drug-specific. Here, we designed a pyrosequencing assay for detect...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2008.08.008
更新日期:2009-01-01 00:00:00
abstract::Seasonal influenza causes significant morbidity and mortality in people aged ≥65 years. Antiviral treatment can reduce complications and disease severity. The objective of this study was to investigate the effect of antiviral treatment in patients aged ≥65 years hospitalized with confirmed influenza in preventing inte...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2020.104785
更新日期:2020-06-01 00:00:00
abstract::Crimean-Congo hemorrhagic fever (CCHF) is a tick-borne viral disease of humans that affects a wide geographic area of Africa and Eurasia, including Turkey, Iran, Pakistan, Afghanistan and Russia. Since the first detection of CCHF cases in Turkey in 2002, more than 9700 patients have been reported, with an overall mort...
journal_title:Antiviral research
pub_type: 历史文章,杂志文章,评审
doi:10.1016/j.antiviral.2015.12.003
更新日期:2016-02-01 00:00:00
abstract::Viramidine, the 3-carboxamidine derivative of ribavirin, was effective against a spectrum of influenza A (H1N1, H3N2 and H5N1) and B viruses in vitro, with the 50% effective concentration (EC50) ranging from 2 to 32 microg/ml. The mean 50% cytotoxic concentration (CC50) in the MDCK cells used in these experiments was ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2005.06.003
更新日期:2005-10-01 00:00:00