Abstract：
:Upon screening synthetic small molecule libraries with the infectious hepatitis C virus (HCV) cell culture system, we identified a benzothiazepinecarboxamide (BTC) scaffold that inhibits HCV. A structure-activity relationship (SAR) study with BTCs was performed, and modifications that led to nanomolar antiviral activity and improved the selective index (CC50/EC50) by more than 1000-fold were identified. In addition, a pharmacophore modeling study determined that the tricyclic core and positive charge on the piperidine moiety were essential for antiviral activity. Furthermore, we demonstrated that BTC interferes with HCV glycoprotein E1/E2-mediated viral entry and the generation of infectious virions by using HCV pseudoparticle and cell culture supernatant transfer assays, respectively. BTC showed potent antiviral activity against HCV genotype 2 (EC50 = 0.01 ± 0.01 μM), but was less potent against a genotype 1/2 chimeric virus (EC50 = 2.71 ± 0.05 μM), which expressed the structural proteins of HCV genotype 1. In summary, we identified, optimized, and characterized novel BTC inhibitors that interfere with early and late steps of the HCV viral life cycle.
journal_name
Antiviral Resjournal_title
Antiviral researchauthors
Kim HY,Kong S,Oh S,Yang J,Jo E,Ko Y,Kim SH,Hwang JY,Song R,Windisch MPdoi
10.1016/j.antiviral.2016.01.010subject
Has Abstractpub_date
2016-05-01 00:00:00pages
39-46eissn
0166-3542issn
1872-9096pii
S0166-3542(16)30012-2journal_volume
129pub_type
杂志文章abstract：:Resveratrol (RV), a polyphenolic natural product present in many plants and fruits, exhibits anti-inflammatory, cardio-protective and anti-proliferative properties. Moreover, RV affects a wide variety of viruses including members of the Herpesviridae family, retroviruses, influenza A virus and polyomavirus by altering...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2012.09.003
更新日期：2012-11-01 00:00:00
abstract：:The essential role of SMAR1 in HIV-1 transcription and LTR driven gene expression suggests SMAR1 as an HIV dependency factor (HDF) and a potential anti-HIV therapeutic target. Here, we report for the first time, anti-HIV activity of 8 novel isothiocyanate (ITC) derivatives that differentially stabilise SMAR1. Out of 8...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2019.104648
更新日期：2020-01-01 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：:Derivatives of beta-lactam antibiotics of the cephalosporin type at 0.02-1 mM concentrations interfered with in vitro replication of two DNA-containing viruses, herpes simplex I and vaccinia, but showed no effects on two RNA-viruses, lymphocytic choriomeningitis virus and vesicular stomatitis virus, or on cell viabili...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/0166-3542(88)90014-9
更新日期：1988-11-01 00:00:00
abstract：:HSV-1 multiplication rates have been shown to vary in different tissues and the rate of multiplication may correlate with susceptibility to antiviral chemotherapy. Herpetic stromal keratitis is a necrotizing condition refractive to antiviral therapy and this lack of antiviral efficacy in stromal disease may be the res...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/0166-3542(91)90041-o
更新日期：1991-01-01 00:00:00
abstract：:A newly synthesized imide derivative of 3-nitro-1,8-naphthalic acid, 5-amino-2-(2-dimethylaminoethyl)benzo-[de]-isoquinolin-1,3-dione (designated M-FA-142), was tested on chick embryo cells against herpes simplex virus type 1 (HSV-1) and vaccinia virus (VV), and on Vero cells against African swine fever virus (ASFV). ...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/0166-3542(84)90018-4
更新日期：1984-08-01 00:00:00
abstract：:Infection with the oncogenic γ-herpesviruses Epstein-Barr virus (EBV) and Kaposi's sarcoma-associated herpesvirus (KSHV) cause several severe malignancies in humans. Inhibition of the lytic replication of EBV and KSHV eliminates the reservoir of persistent infection and transmission, consequently preventing the occurr...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2016.12.002
更新日期：2017-02-01 00:00:00
abstract：BACKGROUND AND AIMS:The combination of tenofovir disoproxil fumarate (TDF) plus emtricitabine (FTC) is used extensively to treat HIV infection and also has potent activity against hepatitis B virus (HBV) infection. The aim of this study was to assess the efficacy and tolerance of TDF + FTC in patients with chronic hepa...
journal_title：Antiviral research
pub_type： 临床试验,杂志文章,多中心研究
doi：10.1016/j.antiviral.2011.07.003
更新日期：2011-10-01 00:00:00
abstract：:Citrusinine-I, a new acridone alkaloid isolated from the root bark of the citrus plant (Rutaceae), exhibited potent activity against herpes simplex virus (HSV) type 1 and type 2 at low concentrations relative to their cytotoxicity; 50% effective concentrations (ED50) of citrusinine-I were 0.56 micrograms/ml and 0.74 m...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/0166-3542(89)90065-x
更新日期：1989-08-01 00:00:00
abstract：:Emergence of drug-resistant human cytomegalovirus (HCMV) strains is a substantial problem during treatment of HCMV infections in immunocompromised patients. The Z-isomers of 2-hydroxymethylcyclopropylidenemethyl adenine (synadenol) and guanine (synguanol) were previously shown to be potent inhibitors of AD169 and Town...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/s0166-3542(02)00129-8
更新日期：2002-12-01 00:00:00
abstract：:The aim of the study was to establish a murine model for sensitive screening of potential compounds with in vitro anti-influenza A virus activity. The evaluation in this in vivo model is based on semi-quantitative detection of viral RNA using one-step reverse transcriptase polymerase chain reaction (RT-PCR). After int...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/s0166-3542(02)00184-5
更新日期：2003-03-01 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：:Childhood exanthema caused by different serotypes of coxsackievirus (CV-A) and enterovirus A71 (EV-A71) has become a serious global health problem; it is commonly known as hand, foot, and mouth disease (HFMD). Current EV-A71 vaccine clinical trials have demonstrated that human antibody responses generated by EV-A71 va...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2016.02.008
更新日期：2016-05-01 00:00:00
abstract：:Novel analogues of the anti-HIV-1 agent TSAO-T, [1-[2',5'-bis-O-(tert- butyldimethylsilyl)-beta-D-ribofuranosyl]thymine]-3'-spiro-5"-(4"-amino- 1",2"-oxathiole-2",2"-dioxide) and its 3-methyl counterpart TSAO-m3T were obtained by modifications at positions 2' or 5' of the sugar moiety. These compounds were evaluated f...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/0166-3542(95)00012-b
更新日期：1995-06-01 00:00:00
abstract：:Since it was discovered as the first human tumor virus in 1964, Epstein-Barr Virus (EBV) is now implicated in several types of malignancies. Accordingly, certain aspects of EBV pathobiology have shown promise in anti-cancer research in developing virus-targeting methods for EBV-associated cancers. The unique role of E...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2019.02.015
更新日期：2019-04-01 00:00:00
abstract：:Argentine hemorrhagic fever is a systemic viral disease caused by Junin virus, with a mortality of 15-30% in untreated individuals. Current specific therapy is highly effective in reducing mortality, and consists of the early administration of immune plasma in defined doses of specific neutralizing antibodies per kg o...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/0166-3542(94)90030-2
更新日期：1994-01-01 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：:Each year, up to 10,000 cases of infections with the flavivirus tick-borne encephalitis (TBE) virus that affect the central nervous system are reported in Europe and Asia. Due to the potentially severe adverse effects of post-exposure prophylaxis with TBE virus hyperimmunoglobulin, TBE can currently only be treated sy...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2011.10.023
更新日期：2012-01-01 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：:Antiviral therapies for chronic hepatitis B virus (HBV) infection that are currently applicable for clinical use are limited to nucleos(t)ide analogs targeting HBV polymerase activity and pegylated interferon alpha (PEG-IFN). Towards establishing an effective therapy for HBV related diseases, it is important to develo...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2017.06.005
更新日期：2017-08-01 00:00:00
abstract：:Lentiviral vectors have been shown to be good candidates for gene transfer protocols; however, prevention of insertional mutagenesis remains problematic. Here we report on the design of a conditionally replicating integrase (IN)-defective lentiviral-hybrid episomal vector in which the insertion of the SV40 promoter/or...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2008.06.015
更新日期：2008-12-01 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：:We have shown previously that prostratin, a non-tumor promoting phorbol ester, inhibits chikungunya virus (CHIKV)-induced cytopathic effects in vitro. Prostratin is a potent activator of protein kinases C (PKC), a family of related serine/threonine kinases that regulate many cellular processes such as proliferation an...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2016.12.020
更新日期：2017-03-01 00:00:00
abstract：:The effect of interferon on the replication of herpes simplex virus types 1 and 2 was studied in two murine macrophage-like cell lines which differ in their ability to synthesize interferon. Higher titers of herpes simplex virus type 1 occurred in PU5-1.8 cell cultures where interferon was not produced than in J774A.1...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/0166-3542(86)90010-0
更新日期：1986-05-01 00:00:00
abstract：BACKGROUND:Cases of sustained-virological response (SVR or cure) after an ultra-short duration (≤27 days) of direct-acting antiviral (DAA)-based therapy, despite HCV being detected at end of treatment (EOT), have been reported. Established HCV mathematical models that predict the treatment duration required to achieve ...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2017.06.019
更新日期：2017-08-01 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
abstract：:Because encapsulation of antiviral drugs in liposomes resulted generally in improved activity against retroviral replication in vivo, the antiviral effects of free-SPC3 and liposome-associated SPC3 were compared in cultured human lymphocytes infected with HIV-1. SPC3 was entrapped in various liposomal formulations, ei...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/s0166-3542(02)00002-5
更新日期：2002-06-01 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：:Favipiravir (T-705) is a new anti-influenza drug approved for human use in Japan and progressing through Phase 3 clinical trials in the U.S. In addition to its potent inhibitory effects against influenza virus infection, the compound has been shown to be broadly active against RNA viruses from 9 different families, in...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2015.07.003
更新日期：2015-09-01 00:00:00
abstract：:In the present study, the protective effect of 1T1, a lambda-carrageenan extracted from the red seaweed Gigartina skottsbergii was evaluated in a murine model of herpes simplex virus type 2 (HSV-2) genital infection. Six to eight-week-old female BALB/c mice were intravaginally inoculated with a lethal dose of HSV-2 (M...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2004.07.001
更新日期：2004-11-01 00:00:00
