scholarly journals Development of Triazoles and Triazolium Salts Based on AZT and Their Anti-Viral Activity against HIV-1

Molecules ◽  
2021 ◽  
Vol 26 (21) ◽  
pp. 6720
Author(s):  
Daniel Machado de Alencar ◽  
Juliana Gonçalves ◽  
Andreia Vieira ◽  
Sofia A. Cerqueira ◽  
Cruz Sebastião ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Click Chemistry ◽  
Experimental Model ◽  
Methyl Iodide ◽  
Infected Cells ◽  
Almost All ◽  
Exposure Prophylaxis ◽  
Methyl Triflate ◽  
Hiv 1 ◽  
Triazolium Salts

We report herein a set of 3′-azido-3′-deoxythymidine (AZT) derivatives based on triazoles and triazolium salts for HIV-1 infection. The compounds were synthesized via click chemistry with Cu(I) and Ru(II) catalysts. Triazolium salts were synthesized by reaction with methyl iodide or methyl triflate in good yields. The antiviral activity of the compounds was tested using two methodologies: In method one the activity was measured on infected cells; in method two a pre-exposure prophylaxis experimental model was employed. For method one the activity of the compounds was moderate, and in general the triazolium salts showed a decreased activity in relation to their triazole precursors. With method two the antiviral activity was higher. All compounds were able to decrease the infection, with two compounds able to clear almost all the infection, while a lower antiviral activity was noted for the triazolium salts. These results suggest that these drugs could play an important role in the development of pre-exposure prophylaxis therapies.

scholarly journals Development of Triazoles based on AZT and their Anti-Viral Activity Against HIV-1

2019 ◽  
Author(s):  
Daniel Alencar ◽  
Juliana Gonçalves ◽  
Sofia A. Cerqueira ◽  
Helena Soares ◽  
Ana Petronilho
Keyword(s):  
Experimental Model ◽  
Viral Activity ◽  
Almost All ◽  
Exposure Prophylaxis ◽  
Hiv 1 ◽  
Hiv1 Infection ◽  
Triazolium Salts

ABSTRACTWe report herein a set of 3’-azido-3’-deoxythymidine (AZT) derivatives based on triazoles and triazolium salts for HIV1 infection. Compounds were tested with □using HIV1 pre-exposure prophylaxis experimental model. All compounds were able to decrease infection and two of them were able to clear almost all the infection, suggesting that these drugs could play an important role in pre-exposure prophylaxis therapies.

Antiviral Properties of the HIV-1 Proteinase Inhibitor RO 31-8959

1994 ◽  
Vol 5 (1) ◽  
pp. 43-45 ◽  
Author(s):  
S. Galpin ◽  
N. A. Roberts ◽  
T. O'Connor ◽  
D. J. Jeffries ◽  
D. Kinchington
Keyword(s):  
Antiviral Activity ◽  
Proteinase Inhibitor ◽  
Potent Inhibitor ◽  
Significant Loss ◽  
Infectious Dose ◽  
Culture Time ◽  
Infected Cells ◽  
Resistant Strains ◽  
Peptide Derivative ◽  
Hiv 1

The peptide derivative Ro 31-8959 has been shown to be a potent inhibitor of HIV proteinase with an IC50 of 2 × 10−9M, against HIV-1RF in acutely infected lymphoblastoid cells. This inhibition was not overcome by increasing the infectious dose or by extending the culture time. Similar antiviral activity was also obtained against HIV-2, SIV and several AZT-resistant strains of HIV-1. The time of addition of the inhibitor could be delayed for 22 h without significant loss of activity, supporting its mode of action as taking place late in the replication cycle of HIV-1. Ro 31-8959 also showed activity against chronically infected cells.

Lipid prodrugs of phosphonoacids: greatly enhanced antiviral activity of 1-O-octadecyl-sn-glycero-3-phosphonoformate in HIV-1, HSV-1 and HCMV-infected cells, in vitro

1996 ◽  
Vol 31 (1-2) ◽  
pp. 59-67 ◽  
Author(s):  
Karl Y. Hostetler ◽  
Ganesh D. Kini ◽  
James R. Beadle ◽  
Kathy A. Aldern ◽  
Michael F. Gardner ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Infected Cells ◽  
Hiv 1 ◽  
Hsv 1

Delivery of double-stranded DNA thioaptamers into HIV-1 infected cells for antiviral activity

2006 ◽  
Vol 344 (3) ◽  
pp. 792-797 ◽  
Author(s):  
Monique R. Ferguson ◽  
Daniel R. Rojo ◽  
Anoma Somasunderam ◽  
Varatharasa Thiviyanathan ◽  
Bettye D. Ridley ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Double Stranded Dna ◽  
Infected Cells ◽  
Hiv 1

TRIM5α Improves CD8+ T-cell Antiviral Activity and Synergize Intrinsic Restriction and Adaptive Immunity in HIV-1 Infected Cells

2014 ◽  
Vol 30 (S1) ◽  
pp. A177-A178
Author(s):  
Esther Jimenez ◽  
Henrik Kloverpis ◽  
Ruth Peña ◽  
Nuria Izquierdo-Useros ◽  
Clotet Bonaventura ◽  
...  
Keyword(s):  
T Cell ◽  
Antiviral Activity ◽  
Adaptive Immunity ◽  
Cd8 T Cell ◽  
Infected Cells ◽  
Hiv 1

scholarly journals Antiviral Activity of CYC202 in HIV-1-infected Cells

2004 ◽  
Vol 280 (4) ◽  
pp. 3029-3042 ◽  
Author(s):  
Emmanuel Agbottah ◽  
Cynthia de La Fuente ◽  
Sergie Nekhai ◽  
Anna Barnett ◽  
Athos Gianella-Borradori ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Infected Cells ◽  
Hiv 1

scholarly journals Antiviral Activity of Genital Tract Secretions After Oral or Topical Tenofovir Pre-exposure Prophylaxis for HIV-1

2014 ◽  
Vol 66 (1) ◽  
pp. 65-73 ◽  
Author(s):  
Betsy C. Herold ◽  
Charlene S. Dezzutti ◽  
Barbra A. Richardson ◽  
Jeanne Marrazzo ◽  
Pedro M. M. Mesquita ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Genital Tract ◽  
Exposure Prophylaxis ◽  
Hiv 1

Phosphatidyl-2′,3′-dideoxy-3′-thiacytidine: synthesis and antiviral activity in hepatitis B- and HIV-1-infected cells

1995 ◽  
Vol 28 (2) ◽  
pp. 113-120 ◽  
Author(s):  
H XIE ◽  
M VORONKOV ◽  
D LIOTTA ◽  
B KORBA ◽  
R SCHINAZI ◽  
...  
Keyword(s):  
Hepatitis B ◽  
Antiviral Activity ◽  
Infected Cells ◽  
Hiv 1

scholarly journals Interferon-induced exonuclease ISG20 exhibits an antiviral activity against human immunodeficiency virus type 1

2005 ◽  
Vol 86 (8) ◽  
pp. 2221-2229 ◽  
Author(s):  
Lucile Espert ◽  
Geneviève Degols ◽  
Yea-Lih Lin ◽  
Thierry Vincent ◽  
Monsef Benkirane ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Antiviral Activity ◽  
Human Immunodeficiency Virus Type ◽  
Antiviral Effect ◽  
Exonuclease Activity ◽  
Immunodeficiency Virus ◽  
Infected Cells ◽  
Induced Apoptosis ◽  
Hiv 1

Interferons (IFNs) encode a family of secreted proteins that provide the front-line defence against viral infections. It was recently shown that ISG20, a new 3′→5′ exoribonuclease member of the DEDD superfamily of exonucleases, represents a novel antiviral pathway in the mechanism of IFN action. In this report, it was shown that ISG20 expression is rapidly and strongly induced during human immunodeficiency virus type 1 (HIV-1) infection. In addition, it was demonstrated that the replication kinetics of an HIV-1-derived virus expressing the ISG20 protein (HIV-1NL4-3ISG20) was delayed in both CEM cells and peripheral blood mononuclear cells. No antiviral effect was observed in cells overexpressing a mutated ISG20 protein defective in exonuclease activity, suggesting that the antiviral effect was due to the exonuclease activity of ISG20. Paradoxically, despite the antiviral activity of ISG20 protein, virus rescue observed in HIV-1NL4-3ISG20-infected cells was not due to mutation or partial deletion of the ISG20 transgene, suggesting that the virus was able to counteract the cellular defences. In addition, HIV-1-induced apoptosis was significantly reduced in HIV-1NL4-3ISG20-infected cells suggesting that emergence of HIV-1NL4-3ISG20 was associated with the inhibition of HIV-1-induced apoptosis. Altogether, these data reflect the ineffectiveness of virus replication in cells overexpressing ISG20 and demonstrate that ISG20 represents a new factor in the IFN-mediated antiviral barrier against HIV-1.

scholarly journals Impacts of Epitope Expression Kinetics and Class I Downregulation on the Antiviral Activity of Human Immunodeficiency Virus Type 1-Specific Cytotoxic T Lymphocytes

2004 ◽  
Vol 78 (2) ◽  
pp. 561-567 ◽  
Author(s):  
Ayub Ali ◽  
Rachel Lubong ◽  
Hwee Ng ◽  
David G. Brooks ◽  
Jerome A. Zack ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Antiviral Activity ◽  
Human Immunodeficiency Virus Type ◽  
Virus Type ◽  
Class I ◽  
Early Protein ◽  
Immunodeficiency Virus ◽  
Infected Cells ◽  
Hiv 1

ABSTRACT The determinants of CD8+ cytotoxic T-lymphocyte (CTL) antiviral activity against human immunodeficiency virus type 1 (HIV-1) remain poorly defined. Although recent technological advances have markedly enhanced the ability to detect HIV-1-specific T cells, commonly used assays do not reveal their direct interaction with virus. We investigated two determinants of CTL antiviral efficiency by manipulating HIV-1 and measuring the effects on CTL suppression of viral replication in acutely infected cells. Translocation of a Gag epitope into the early protein Nef markedly increased the activity of CTL recognizing that epitope, in comparison to HIV-1 expressing the epitope normally in the late protein Gag. Because this epitope translocation resulted not only in earlier expression but also in loss of major histocompatibility complex class I downregulation by Nef, the activities of CTL against a panel of viral constructs differing in kinetics of epitope expression and class I downmodulation were compared. The results indicated that both the timing of epitope expression and the reduction of class I have profound effects on the ability of CTL to suppress HIV-1 replication in acutely infected cells. The epitope targeting of CTL and viral control of class I therefore likely play important roles in the ability of CTL to exert pressure on HIV-1.

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