Abstract
A series of novel mono-1,2,3-triazole and bis-1,2,3-triazole acyclonucleoside analogues of 9-(4-hydroxybutyl)guanine was prepared via copper(I)-catalyzed 1,3-dipolar cycloaddition of N-9 propargylpurine, N-1-propargylpyrimidines/as-triazine with the azido-pseudo-sugar 4-azidobutylacetate under solvent-free microwave conditions, followed by treatment with K2CO3/MeOH, or NH3/MeOH. All compounds studied in this work were screened for their antiviral activities [against human rhinovirus (HRV) and hepatitis C virus (HCV)] and antibacterial activities against a series of Gram positive and negative bacteria.
Highlights
For several years, there has been an intensive search for drugs effective in chemotherapy of viral diseases like AIDS, herpes simplex, Hepatitis C and cytomegaloviruses [1,2,3,4,5]
In the light of these findings and in continuation of our previous investigation [34], we considered the synthesis of new 1,2,3-triazole and bis-1,2,3-triazole acyclonucleosides
The antibacterial activity of all the synthesized compounds 10a–d and 12a–c were examined against different Gram-positive Staphylococcus aureus (ATCC 13709 in vivo, ATCC 25923, oxford and MRSA in vivo), Enterococcus faecalis (ATCC 29212 VanS), Enterococcus faecium (VanA), Streptococcus pneumoniae (VanA, ATCC49619, PenR and Blood effect), and Gram-negative
Summary
There has been an intensive search for drugs effective in chemotherapy of viral diseases like AIDS, herpes simplex, Hepatitis C and cytomegaloviruses [1,2,3,4,5]. Most of these drugs are analogues of naturally occurring nucleosides [6]. Many variations were tested in order to enhance biological activity and selectivity, or to lower toxicity [13,14,15,16,17,18]. Among them HBG [9-(4-hydroxybutyl)guanine] (2, Figure 1) presented good activity against HSV-1 and HSV-2
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