Thiazolidinone–Peptide Hybrids as Dengue Virus Protease Inhibitors with Antiviral Activity in Cell Culture

2013 ◽  
Vol 56 (21) ◽  
pp. 8389-8403 ◽  
Author(s):  
Christoph Nitsche ◽  
Verena N. Schreier ◽  
Mira A. M. Behnam ◽  
Anil Kumar ◽  
Ralf Bartenschlager ◽  
...  
Keyword(s):  
Cell Culture ◽  
Antiviral Activity ◽  
Dengue Virus ◽  
Protease Inhibitors

Synthesis and biological evaluation of α-ketoamides as inhibitors of the Dengue virus protease with antiviral activity in cell-culture

2011 ◽  
Vol 19 (13) ◽  
pp. 4067-4074 ◽  
Author(s):  
Christian Steuer ◽  
Christian Gege ◽  
Wolfgang Fischl ◽  
Karl H. Heinonen ◽  
Ralf Bartenschlager ◽  
...  
Keyword(s):  
Cell Culture ◽  
Antiviral Activity ◽  
Dengue Virus ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

scholarly journals 4,7-Disubstituted 7H-Pyrrolo[2,3-d]pyrimidines and Their Analogs as Antiviral Agents against Zika Virus

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3779
Author(s):  
Ruben Soto-Acosta ◽  
Eunkyung Jung ◽  
Li Qiu ◽  
Daniel J. Wilson ◽  
Robert J. Geraghty ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Dengue Virus ◽  
Small Molecules ◽  
Zika Virus ◽  
Antiviral Agents ◽  
Structural Features ◽  
Molecular Target ◽  
Core Structure ◽  
Human Pathogens ◽  
Important Group

Discovery of compound 1 as a Zika virus (ZIKV) inhibitor has prompted us to investigate its 7H-pyrrolo[2,3-d]pyrimidine scaffold, revealing structural features that elicit antiviral activity. Furthermore, we have demonstrated that 9H-purine or 1H-pyrazolo[3,4-d]pyrimidine can serve as an alternative core structure. Overall, we have identified 4,7-disubstituted 7H-pyrrolo[2,3-d]pyrimidines and their analogs including compounds 1, 8 and 11 as promising antiviral agents against flaviviruses ZIKV and dengue virus (DENV). While the molecular target of these compounds is yet to be elucidated, 4,7-disubstituted 7H-pyrrolo[2,3-d]pyrimidines and their analogs are new chemotypes in the design of small molecules against flaviviruses, an important group of human pathogens.

Antiviral activity of uridine 5′-diphosphate glucose analogues against some enveloped viruses in cell culture

1987 ◽  
Vol 8 (5-6) ◽  
pp. 299-310 ◽  
Author(s):  
G. Gil-Fernández ◽  
S. Pérez ◽  
P. Vilas ◽  
C. Pérez ◽  
F.G. de las Heras ◽  
...  
Keyword(s):  
Cell Culture ◽  
Antiviral Activity ◽  
Enveloped Viruses ◽  
Glucose Analogues ◽  
Diphosphate Glucose

In Vitro Antiviral Activity of Pinus merkusii (Pinaceae) Stem Bark and Cone against Dengue Virus Type-2 (DENV-2)

2021 ◽  
pp. 3705-3708
Author(s):  
Arif Nur Muhammad Ansori ◽  
Amaq Fadholly ◽  
Annise Proboningrat ◽  
Suhailah Hayaza ◽  
Raden Joko Kuncoroningrat Susilo ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Dengue Virus ◽  
Virus Type ◽  
Stem Bark ◽  
Endemic Region ◽  
In Vivo Evaluation ◽  
African Green Monkey Kidney ◽  
Antiviral Compound ◽  
Dengue Virus Type 2

Dengue is a major mosquito-borne disease that currently has no effective antiviral or vaccine available. Recently, Indonesia is one of the largest countries in the dengue-endemic region, with a total population of more than 250 million. In the present study, the antiviral activity of P. merkusii stem bark and cone were evaluated against dengue virus type-2 (DENV-2; NCBI accession number: KT012509) isolated from Surabaya, Indonesia. We revealed that P. merkusii stem bark and cone inhibited DENV-2 in Vero cells (originally from African green monkey kidney) with IC50= 140.63 μg/mL and 73.78 μg/mL, CC50= 89.65 μg/mL and 249.5 μg/mL, SI= 0.64 and 3.38, respectively. The findings presented here suggest that P. merkusii stem bark and cone exerts potent antiviral activity against DENV-2. Hence, P. merkusii stem bark and cone are potent to inhibit DENV-2 and should be considered for in vivo evaluation in the development of an effective antiviral compound against DENV-2.

Pyrrolinone-Based HIV Protease Inhibitors. Design, Synthesis, and Antiviral Activity: Evidence for Improved Transport

1995 ◽  
Vol 117 (45) ◽  
pp. 11113-11123 ◽  
Author(s):  
Amos B Smith ◽  
Ralph Hirschmann ◽  
Alexander Pasternak ◽  
Mark C. Guzman ◽  
Akihisa Yokoyama ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Protease Inhibitors ◽  
Hiv Protease ◽  
Hiv Protease Inhibitors ◽  
Design Synthesis

scholarly journals In vitro activity of human recombinant alpha-2b interferon against SARS-CoV-2 virus

2021 ◽  
Vol 66 (2) ◽  
pp. 123-128
Author(s):  
S. Ya. Loginova ◽  
V. N. Shсhukina ◽  
S. V. Savenko ◽  
S. V. Borisevich
Keyword(s):  
Cell Culture ◽  
Antiviral Activity ◽  
Viral Infections ◽  
Complete Suppression ◽  
Antiviral Efficacy ◽  
Prevention And Treatment ◽  
Proven Efficacy ◽  
High Antiviral Activity

Introduction. The pandemic spread of a new coronavirus infection, COVID-19, has caused a global emergency and attracted the attention of public health professionals and the population of all countries. A significant increase in the number of new cases of SARS-CoV-2 infection demonstrates the urgency of finding drugs effective against this pathogen.The aim of this work was to evaluate the in vitro antiviral efficacy of human recombinant alpha-2b interferon (IFN-α2b) against SARS-CoV-2 virus.Material and methods. The experiments had been carried out on Vero Cl008, the continuous line of African green monkey (Chlorocebus sabaeus) kidney cells. The effectiveness of the drugs was assessed by the suppression of viral reproduction in vitro. The biological activity was determined using titration of a virus-containing suspension in a Vero Cl008 cell culture by the formation of negative colonies.Results. The antiviral efficacy of the IFN-α2b-based medications, which have a high safety profile and proven efficacy in the prevention and treatment of influenza and acute respiratory viral infections (ARVI), has been studied against the new pandemic SARS-CoV-2 virus in vitro experiments in Vero C1008 cell culture. IFN-α2b effectively inhibits the reproduction of the virus when applied both 24 hrs before and 2 hrs after infection. In the IFN-α2b concentration range 102–106 IU/ml a complete suppression of the reproduction of the SARS-CoV-2 virus had been demonstrated.Discussion. IFN-α2b demonstrated in vitro high antiviral activity against SARS-CoV-2. In addition, the substance has a high chemotherapeutic index (>1000).Conclusion. Medications for intranasal use based on IFN-α2b have high antiviral activity and are promising drugs for in vivo study in terms of prevention and treatment of COVID-19.

Antiviral activity of Faramea bahiensis leaves on dengue virus type-2 and characterization of a new antiviral flavanone glycoside

2017 ◽  
Vol 19 ◽  
pp. 220-225 ◽  
Author(s):  
Adriana C. Nascimento ◽  
Ligia M.M. Valente ◽  
Mário Gomes ◽  
Rodolfo S. Barboza ◽  
Thiago Wolff ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Dengue Virus ◽  
Virus Type ◽  
Flavanone Glycoside ◽  
Dengue Virus Type 2

HIV-1 Protease Inhibitors with a Transition-State Mimic Comprising a Tertiary Alcohol: Improved Antiviral Activity in Cells

2010 ◽  
Vol 53 (2) ◽  
pp. 607-615 ◽  
Author(s):  
A.K. Mahalingam ◽  
Linda Axelsson ◽  
Jenny K. Ekegren ◽  
Johan Wannberg ◽  
Jacob Kihlström ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Transition State ◽  
Protease Inhibitors ◽  
Tertiary Alcohol ◽  
Hiv 1 ◽  
In Cells

Zinc finger protein ZFP36L1 inhibits flavivirus infection by both 5′-3′ XRN1 and 3′-5′ RNA-exosome RNA decay pathways.

2021 ◽  
Author(s):  
Han Chiu ◽  
Hsin-Ping Chiu ◽  
Han-Pang Yu ◽  
Li-Hsiung Lin ◽  
Zih-Ping Chen ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Dengue Virus ◽  
Zinc Finger ◽  
Rna Binding ◽  
Zinc Finger Protein ◽  
Viral Rna ◽  
Rna Decay ◽  
Finger Protein ◽  
Zinc Finger Motifs ◽  
Rna Exosome

Zinc-finger protein 36, CCCH type-like 1 (ZFP36L1), containing tandem CCCH-type zinc-finger motifs with an RNA-binding property, plays an important role in cellular RNA metabolism mainly via RNA decay pathways. Recently, we demonstrated that human ZFP36L1 has potent antiviral activity against influenza A virus infection. However, its role in the host defense response against flaviviruses has not been addressed. Here, we demonstrate that ZFP36L1 functions as a host innate defender against flaviviruses, including Japanese encephalitis virus (JEV) and dengue virus (DENV). Overexpression of ZFP36L1 reduced JEV and DENV infection, and ZFP36L1 knockdown enhanced viral replication. ZFP36L1 destabilized the JEV genome by targeting and degrading viral RNA mediated by both 5′-3′ XRN1 and 3′-5′ RNA-exosome RNA decay pathways. Mutation in both zinc-finger motifs of ZFP36L1 disrupted RNA-binding and antiviral activity. Furthermore, the viral RNA sequences specifically recognized by ZFP36L1 were mapped to the 3'-untranslated region of the JEV genome with the AU-rich element (AUUUA) motif. We extend the function of ZFP36L1 to host antiviral defense by directly binding and destabilizing the viral genome via recruiting cellular mRNA decay machineries. Importance Cellular RNA-binding proteins are among the first lines of defense against various viruses, particularly RNA viruses. ZFP36L1 belongs to the CCCH-type zinc-finger protein family and has RNA-binding activity; it has been reported to directly bind to the AU-rich elements (AREs) of a subset of cellular mRNAs and then lead to mRNA decay by recruiting mRNA degrading enzymes. However, the antiviral potential of ZFP36L1 against flaviviruses has not yet been fully demonstrated. Here, we reveal the antiviral potential of human ZFP36L1 against Japanese encephalitis virus (JEV) and dengue virus (DENV). ZFP36L1 specifically targeted the ARE motif within viral RNA and triggered the degradation of viral RNA transcripts via cellular degrading enzymes, 5′-3′ XRN1 and 3′-5′ RNA exosome. These findings provide mechanistic insights into how human ZFP36L1 serves as a host antiviral factor to restrict flavivirus replication.

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