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 strain), and West Nile viruses. One of the most interesting molecules, compound 16, showed broad antiviral activity against additional flaviviruses such as Dengue 1, 3 and 4, Zika, Japanese encephalitis, several strains of Yellow fever, and tick-borne encephalitis viruses. Compound 16 did not exert any effect on alphaviruses and phleboviruses and its activity was maintained in YFV infected cells from different species. The activity of 16 appears specific for flavivirus with respect to other virus families, suggesting, but not proving, that it might be targeting a viral factor. We demonstrated that the antiviral effect of 16 is not related to reduced viral RNA synthesis or virion release. On the contrary, viral particles grown in the presence of 16 showed reduced infectivity, being unable to perform a second round of infection. The chemical class herein presented thus emerges as suitable to provide pan-flavivirus inhibitors.
journal_name
Antiviral Resjournal_title
Antiviral researchauthors
Cannalire R,Tarantino D,Piorkowski G,Carletti T,Massari S,Felicetti T,Barreca ML,Sabatini S,Tabarrini O,Marcello A,Milani M,Cecchetti V,Mastrangelo E,Manfroni G,Querat Gdoi
10.1016/j.antiviral.2019.03.004subject
Has Abstractpub_date
2019-07-01 00:00:00pages
6-12eissn
0166-3542issn
1872-9096pii
S0166-3542(18)30738-1journal_volume
167pub_type
杂志文章abstract：BACKGROUND AND AIMS:Interferon-alpha treatment has been the treatment of choice for chronic hepatitis with unpredictable results. Recently, Lamivudine has been licensed for use against HBV infection with good results. Unfortunately, recurrence of viremia after lamivudine withdrawal is common and prolonged treatment can...
journal_title：Antiviral research
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1016/s0166-3542(00)00141-8
更新日期：2001-02-01 00:00:00
abstract：:Rotavirus infection has emerged as an important cause of complications in organ transplantation recipients and might play a role in the pathogenesis of inflammatory bowel disease (IBD). 6-Thioguanine (6-TG) has been widely used as an immunosuppressive drug for organ recipients and treatment of IBD in the clinic. This ...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2018.06.011
更新日期：2018-08-01 00:00:00
abstract：:Rabies is a lethal viral infection that can affect almost all mammals, including humans. To better understand the replication of Rabies lyssavirus, we investigated if the viral load in brains naturally infected with rabies influences viral internalization and viral growth kinetics in neuroblastoma cells, and if the vi...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2017.11.003
更新日期：2018-01-01 00:00:00
abstract：:Commercial vaccines against human papillomavirus (HPV) have low uptake due to parental autonomy, dosing regimen, cost, and cold chain storage requirements. Carrageenan (CG)-based formulations prevent HPV infection in vitro and in vivo but data are needed on the durability of anti-HPV activity and the effect of seminal...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2014.05.018
更新日期：2014-08-01 00:00:00
abstract：:Amyotrophic lateral sclerosis (ALS) is a progressive, invariably fatal neurologic disorder resulting from upper and lower motor neuron degeneration, which typically develops during the sixth or seventh decade of life, and is diagnosed based on standard clinical criteria. Its underlying cause remains undetermined. The ...
journal_title：Antiviral research
pub_type： 杂志文章,评审
doi：10.1016/j.antiviral.2013.05.006
更新日期：2013-08-01 00:00:00
abstract：:In March and April 2009, an entirely novel influenza A (H1N1) virus (NIAV) emerged in Mexico and the USA. During the subsequent months, the virus rapidly spread all over the world by person-to-person transmission. In this report, RNA interference (RNAi) was used as an antiviral agent to inhibit NIAV replication in A54...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2009.12.010
更新日期：2010-03-01 00:00:00
abstract：:Prunellin, an anti-HIV active compound, was isolated from aqueous extracts of the Chinese medicinal herb, Prunella vulgaris, and purified to chromatographic homogeneity. Infrared and NMR spectroscopy identified prunellin as a polysaccharide. Elemental analyses, precipitation with calcium(II), barium(II), or 9-aminoacr...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/0166-3542(89)90036-3
更新日期：1989-06-01 00:00:00
abstract：:Therapeutic strategies controlling human cytomegalovirus (hCMV) infection are limited due to adverse side effects and emergence of antiviral resistance variants. A compound being evaluated for treating hCMV disease is maribavir (MBV) which disrupts replication by inhibiting the viral kinase pUL97. Previous studies hav...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2013.09.011
更新日期：2013-11-01 00:00:00
abstract：:Carbohydrate-binding proteins (CBP) can be isolated from a variety of species, including procaryotes (i.e. cyanobacteria), sea corals, algae, plants, invertebrates and vertebrates. A number of them, in particular those CBP that show specific recognition for mannose (Man) and N-acetylglucosamine (GlcNAc) are endowed wi...
journal_title：Antiviral research
pub_type： 杂志文章,评审
doi：10.1016/j.antiviral.2006.02.004
更新日期：2006-09-01 00:00:00
abstract：:Oxymatrine (OMTR) is an anti-hepatitis drug used in China. Its mechanism of action is unknown. Recently, we found that OMTR inhibits hepatitis B virus (HBV) via down-regulating the expression of heat-stress cognate 70 (Hsc70), a host protein required for HBV DNA replication. Goal of this study was to assess the effect...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2011.01.005
更新日期：2011-03-01 00:00:00
abstract：:IRES-driven translation plays an essential role in picornavirus infection. However, there are seldom reports of compounds targeting this pathway with effective protection in animal models. Here, we identified emetine, an antiprotozoal drug, which inhibits EV-A71 with an EC50 value of 0.04 μM and a CC50 value of 10 μM ...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2019.104650
更新日期：2020-01-01 00:00:00
abstract：:The present study was undertaken to examine the potential of rectal route of immunization for induction of protective immunity in the female genital tract against genital herpes infection in mice. A single rectal immunization of female C57Bl/6 mice with live attenuated herpes simplex virus type 2 lacking thymidine kin...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2007.12.014
更新日期：2008-06-01 00:00:00
abstract：:The influenza A (H1N1) virus is a highly contagious acute respiratory disease affecting pigs and humans. This disease causes severe economic loss in many countries, and developing mucosal vaccines is an efficient strategy to control the influenza virus. The neonatal Fc receptor (FcRn) plays an important role in transf...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2016.11.025
更新日期：2017-02-01 00:00:00
abstract：:Flavivirus methyltransferase is a genetically-validated antiviral target. Crystal structures of almost all available flavivirus methyltransferases contain S-adenosyl-L-methionine (SAM), the methyl donor molecule that co-purifies with the enzymes. This raises a possibility that SAM is an integral structural component r...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2014.09.003
更新日期：2014-11-01 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：:Oligodeoxynucleotides (ODNs) composed entirely of deoxyguanosine and thymidine, but not specifically designed to act as antisense agents, were able to significantly inhibit herpes simplex virus growth in acute infection assay systems. The guanosine/thymidine (GT) ODNs which demonstrated this antiviral activity contain...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/0166-3542(94)00064-f
更新日期：1995-01-01 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：:Nucleic acid polymers (NAPs) block the release of HBsAg from infected hepatocytes. These compounds have been previously shown to have the unique ability to eliminate serum surface antigen in DHBV-infected Pekin ducks and achieve multilog reduction of HBsAg or HBsAg loss in patients with chronic HBV infection and HBV/H...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2017.10.022
更新日期：2018-01-01 00:00:00
abstract：:Isolation of rhinoviruses from nasal secretions may be delayed or prevented by exogenously applied interferon which is carried over into nasal wash specimens. In studies of interferon-alpha 2 treated volunteers with experimental rhinovirus infection, we determined that incorporation of antiinterferon antibody into col...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/0166-3542(83)90016-5
更新日期：1983-03-01 00:00:00
abstract：:Suberoylanilide hydroxamic acid (SAHA) has been assessed in clinical trials as part of a "shock and kill" strategy to cure HIV-infected patients. While it was effective at inducing expression of HIV RNA ("shock"), treatment with SAHA did not result in a reduction of reservoir size ("kill"). We therefore utilized a com...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2015.09.002
更新日期：2015-11-01 00:00:00
abstract：:A series of phosphoramidate derivatives of the anti-HIV drug AZT has been prepared as membrane soluble pro-drugs of the bio-active nucleotide forms and evaluated in vitro against HIV-1. Terminal substituted alkyl amines have a pronounced anti-HIV effect: this effect declines upon increasing the length of the methylene...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/0166-3542(90)90053-a
更新日期：1990-12-01 00:00:00
abstract：:Innate, non-specific, resistance mechanisms are important barriers to pathogens, particularly delaying virus multiplication at the onset of infections. These innate defense mechanisms include a series of mechanical barriers, pre-existing inhibitory molecules, and cellular responses with antimicrobial activity. The ant...
journal_title：Antiviral research
pub_type： 杂志文章,评审
doi：10.1016/s0166-3542(00)00126-1
更新日期：2000-11-01 00:00:00
abstract：:Viracea, a topical microbicide, is a blend of benzalkonium chloride and phytochemicals derived from Echinacea purpurea and is a proprietary formula from Destiny BioMediX Corp. Viracea was tested against 40 strains of herpes simplex virus (HSV): 15 strains (five HSV-1 and ten HSV-2) were resistant to acyclovir (ACV-R) ...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/s0166-3542(98)00027-8
更新日期：1998-07-01 00:00:00
abstract：:Natural products provide a large reservoir of potentially active agents with anti-hepatitis B virus (HBV) activity. We examined the effect of the polyphenolic extract from Geranium carolinianum L. (PPGC) on HBV replication both in vitro and in vivo. In the human HBV-transfected liver cell line HepG(2) 2.2.15, PPGC eff...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2008.03.001
更新日期：2008-08-01 00:00:00
abstract：:Carbovir (CBV) is a guanine nucleoside analog with potent in vitro anti-HIV activity. A prodrug of CBV is currently being evaluated in clinical trials as a potential agent for the treatment of AIDS. The ability of CBV to inhibit mitochondrial DNA synthesis in intact CEM cells was evaluated in the present study, becaus...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/s0166-3542(97)01033-4
更新日期：1997-05-01 00:00:00
abstract：:To identify monoclonal antibodies (mAbs) with high potency and novel recognition sites, more than 25,000 of mouse hybridomas were screened and 4 novel anti-human CCR5 mAbs ROAb12, ROAb13, ROAb14, and ROAb18 showing potent activity in cell-cell fusion (CCF) assay were identified. These mAbs demonstrated potent antivira...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2006.11.003
更新日期：2007-05-01 00:00:00
abstract：:Several nucleoside reverse transcriptase inhibitors are associated with mitochondrial toxicity resulting from inhibition of DNA polymerase-gamma. This study compared the effects on mitochondrial DNA of apricitabine (previously referred to as AVX754 or SPD754), a novel cytidine analogue under development for the treatm...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2007.05.004
更新日期：2007-10-01 00:00:00
abstract：:Tiazofurine (2-beta-D-ribofuranosylthiazole-4-carboxamide) was found to inhibit replication of barley stripe mosaic virus (BSMV) in barley and wheat plants. Treatment with this nucleoside analogue delayed and inhibited symptom development and suppressed virus multiplication. The most effective concentration applied tw...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/0166-3542(89)90019-3
更新日期：1989-02-01 00:00:00
abstract：:Transcriptional activation of HIV-1 gene expression is partially controlled by the interaction between viral and cellular transcription factors acting at HIV-1 long terminal repeat (LTR) sequences. HIV-1 subtyping at LTR region and nucleotide LTR variability from clinical samples in 48 subjects carrying different HIV-...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2010.08.007
更新日期：2010-11-01 00:00:00
abstract：:Natural compounds provide a large reservoir of potentially active anti-hepatitis B virus (HBV) agents. We examined the direct effects of protocatechuic aldehyde (PA; derived from the Chinese herb, Salvia miltiorrhiza) on HBV replication in HepG2 2.2.15 cell line and duck hepatitis B virus (DHBV) replication in ducklin...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2006.12.005
更新日期：2007-04-01 00:00:00
