Synthesis and antiviral activity of an imidazo[1,2-a]pyrrolo[2,3-c]pyridine series against the bovine viral diarrhea virus

2010 ◽  
Vol 45 (5) ◽  
pp. 2044-2047 ◽  
Author(s):  
Jean-Michel Chezal ◽  
Jan Paeshuyse ◽  
Vincent Gaumet ◽  
Damien Canitrot ◽  
Aurélie Maisonial ◽  
...  
2020 ◽  
Vol 157 ◽  
pp. 569-576
Author(s):  
Laura Junqueira de Camargo ◽  
Tony Picoli ◽  
Geferson Fischer ◽  
Ana Claudia Oliveira de Freitas ◽  
Rodrigo Bozembecker de Almeida ◽  
...  

2008 ◽  
Vol 89 (4) ◽  
pp. 1000-1009 ◽  
Author(s):  
Spencer Hoover ◽  
Rob Striker

The family Flaviviridae comprises positive-strand RNA viral pathogens of humans and livestock with few treatment options. We have previously shown that azathioprine (AZA) has in vitro activity against bovine viral diarrhea virus (BVDV). While the mechanism of inhibition is unknown, AZA and related thiopurine nucleoside analogues have been used as immunosuppressants for decades and both AZA metabolites and cellular genes involved in AZA metabolism have been extensively characterized. Here, we show that only certain riboside metabolites have antiviral activity and identify the most potent known antiviral AZA metabolite as 6-methylmercaptopurine riboside (6MMPr). The antiviral activity of 6MMPr is antagonized by adenosine, and is specific to BVDV and not to the related yellow fever virus. An essential step in the conversion of AZA to 6MMPr is the addition of a methyl group onto the sulfur atom attached to position six of the purine ring. Intracellularly, the methyl group is added by thiopurine methyltransferase (TPMT), an S-adenosyl methionine-dependent methyltransferase. Either chemically bypassing or inhibiting TPMT modulates antiviral activity of AZA metabolites. TPMT exists in several variants with varying levels of activity and since 6MMPr is a potent antiviral, the antiviral activity of AZA may be modulated by host genetics.


Chemotherapy ◽  
2002 ◽  
Vol 48 (3) ◽  
pp. 144-147 ◽  
Author(s):  
M.J. Ruffa ◽  
M. Perusina ◽  
V. Alfonso ◽  
M.L. Wagner ◽  
M. Suriano ◽  
...  

2021 ◽  
pp. 1-10
Author(s):  
Anjuman Ara Bhuyan ◽  
Ali Akbar Bhuiyan ◽  
Atta Muhammad Memon ◽  
Bingzhou Zhang ◽  
Jahangir Alam ◽  
...  

2015 ◽  
Vol 2015 ◽  
pp. 1-9 ◽  
Author(s):  
Marina Aiello Padilla ◽  
Rodney Alexandre Ferreira Rodrigues ◽  
Juliana Cristina Santiago Bastos ◽  
Matheus Cavalheiro Martini ◽  
Ana Caroline de Souza Barnabé ◽  
...  

Extracts from termite-associated bacteria were evaluated forin vitroantiviral activity against bovine viral diarrhea virus (BVDV). Two bacterial strains were identified as active, with percentages of inhibition (IP) equal to 98%. Both strains were subjected to functional analysis via the addition of virus and extract at different time points in cell culture; the results showed that they were effective as posttreatments. Moreover, we performed MTT colorimetric assays to identify the CC50, IC50, and SI values of these strains, and strain CDPA27 was considered the most promising. In parallel, the isolates were identified asStreptomycesthrough 16S rRNA gene sequencing analysis. Specifically, CDPA27 was identified asS. chartreusis. The CDPA27 extract was fractionated on a C18-E SPE cartridge, and the fractions were reevaluated. A 100% methanol fraction was identified to contain the compound(s) responsible for antiviral activity, which had an SI of 262.41. GC-MS analysis showed that this activity was likely associated with the compound(s) that had a peak retention time of 5 min. Taken together, the results of the present study provide new information for antiviral research using natural sources, demonstrate the antiviral potential ofStreptomyces chartreusiscompounds isolated from termite mounds against BVDV, and lay the foundation for further studies on the treatment of HCV infection.


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