Synthesis of a Novel Class of 1,3-oxathiolane Nucleoside Derivatives of T- 705 and Evaluation of Their Anti-influenza A Virus and Anti-HIV Activity

2018 ◽  
Vol 14 (6) ◽  
pp. 595-603 ◽  
Author(s):  
Mingming Han ◽  
Xu Zhao ◽  
Xuedong Wu ◽  
Wei Huang ◽  
Xingzhou Li ◽  
...  
MedChemComm ◽  
2017 ◽  
Vol 8 (5) ◽  
pp. 960-963 ◽  
Author(s):  
A. S. Sokolova ◽  
O. I. Yarovaya ◽  
M. D. Semenova ◽  
A. A. Shtro ◽  
I. R. Orshanskaya ◽  
...  

Herein, we present the design and synthesis of a series of novel heterocyclic derivatives of (−)-borneol and (−)-isoborneol as potent inhibitors of the influenza A virus.


2018 ◽  
Vol 352 (2) ◽  
pp. 1800225 ◽  
Author(s):  
Anastasia V. Galochkina ◽  
Rakesh K. Bollikanda ◽  
Vladimir V. Zarubaev ◽  
Dmitry G. Tentler ◽  
Irina N. Lavrenteva ◽  
...  

2013 ◽  
Vol 100 (1) ◽  
pp. 90-97 ◽  
Author(s):  
Ewelina Krol ◽  
Ilona Wandzik ◽  
Beata Gromadzka ◽  
Dawid Nidzworski ◽  
Malgorzata Rychlowska ◽  
...  

2012 ◽  
Vol 8 ◽  
pp. 705-711 ◽  
Author(s):  
Christian Stanetty ◽  
Andrea Wolkerstorfer ◽  
Hassan Amer ◽  
Andreas Hofinger ◽  
Ulrich Jordis ◽  
...  

The influenza virus infection remains a significant threat to public health and the increase of antiviral resistance to available drugs generates an urgent need for new antiviral compounds. Starting from the natural, antivirally active compound glycyrrhizin, spacer-bridged derivatives were generated with improved antiviral activity against the influenza A virus infection. Simplified analogues of the triterpene saponin glycyrrhizin containing 1-thio-β-D-glucuronic acid residues have been prepared in good yields by alkylation of 3-amino and 3-thio derivatives of glycyrrhetinic acid with a 2-iodoethyl 1-thio-β-D-glucopyranosiduronate derivative. The spacer-connected 3-amino derivatives were further transformed into N-acetylated and N-succinylated derivatives. The deprotected compounds containing these carboxylic acid appendices mimic the glycon part of glycyrrhizin as well as the hemisuccinate derivative of glycyrrhetinic acid, carbenoxolone. Antiviral activities of the compounds were determined in a biological test based on influenza A virus-infected cells, wherein the 3-(2-thioethyl)-N-acetylamino- and 3-(2-thioethyl)-thio-linked glucuronide derivatives were effective inhibitors with IC50 values as low as 54 µM.


2000 ◽  
Vol 74 (10) ◽  
pp. 4505-4511 ◽  
Author(s):  
Ligia A. Pinto ◽  
Vesna Blazevic ◽  
Bruce K. Patterson ◽  
C. Mac Trubey ◽  
Matthew J. Dolan ◽  
...  

ABSTRACT It is now recognized that, in addition to drug-mediated therapies against human immunodeficiency virus type 1 (HIV-1), the immune system can exert antiviral effects via CD8+ T-cell-generated anti-HIV factors. This study demonstrates that (i) supernatants from peripheral blood mononuclear cells (PBMC) stimulated with influenza A virus inhibit replication of CCR5- and CXCR4-tropic HIV-1 isolates prior to reverse transcription; (ii) the HIV-suppressive supernatants can be generated by CD4- or CD8-depleted PBMC; (iii) this anti-HIV activity is partially due to alpha interferon (IFN-α), but not to IFN-γ, IFN-β, the β-chemokines MIP-1α, MIP-1β, and RANTES, or interleukin-16; (iv) the anti-HIV activity is generated equally well by PBMC cultured with either infectious or UV-inactivated influenza A virus; and (v) the antiviral activity can be generated by influenza A-stimulated PBMC from HIV-infected individuals. These findings represent a novel mechanism for inhibition of HIV-1 replication that differs from the previously described CD8 anti-HIV factors (MIP-1α, MIP-1β, RANTES, and CD8 antiviral factor).


2014 ◽  
Vol 22 (24) ◽  
pp. 6826-6836 ◽  
Author(s):  
Anna A. Shtro ◽  
Vladimir V. Zarubaev ◽  
Olga A. Luzina ◽  
Dmitry N. Sokolov ◽  
Oleg I. Kiselev ◽  
...  

2020 ◽  
Author(s):  
Yu-Jen Chang ◽  
Cheng-Yun Yeh ◽  
Ju-Chien Cheng ◽  
Yu-Qi Huang ◽  
Kai-Cheng Hsu ◽  
...  

Abstract Influenza A virus (IAV) is hard to eradicate due to its genetic drift and reassortment ability. Neuraminidase (NA), frequently the target protein, cleaves the sialic acid (SA) and discharges virions to complete the infectious cycle. However, the increasing use of NA inhibitors aroused drug resistance in recent years. Hemagglutinin (HA), on the opposite, initiates the infectious cycle and sticks virions to cells by connecting to the host SA so that HA might be a tempting target. In this study, HA was chosen for SA-binding site model preparation to screen more than 200,000 compounds by molecular docking method in silico. According to the post-screening analysis by iGemdock and SiMMap, nine of the top twenty compounds based on the ranking score were purchased and evaluated. NSC85561 was initially identified from the compounds through the bioassays. Next, the twelve derivatives of NSC85561 were selected to consolidate the primary results. NSC85561 and two of its derivatives were finally identified as potent HA inhibitors by cell proliferation, plaque reduction, and hemagglutination inhibition assays in vitro. These results suggested that virtual screening may be a powerful tool to concise the compounds from the massive database and reduce the complicated bioassays.


Planta Medica ◽  
2012 ◽  
Vol 78 (11) ◽  
Author(s):  
A Derksen ◽  
W Hafezi ◽  
A Hensel ◽  
J Kühn

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