Abstract

We describe the synthesis and the antibacterial evaluation 2’,N3-cyclonucleoside 3 analogue of MTA that is characterized by the presence of an additional linkage between the heterocyclic ring and the sugar moiety.

Highlights

  • During the last few years, physicians have been faced with little solutions to care bacterial infections and in particular those due to the advent of resistant bacteria such as MRSA [1,2,3]

  • The recovery of 5’-deoxy-5’-methyl-thioadenosine and S-adenosylhomocysteine through the Sadenosylmethionine metabolic pathway is crucial to mammals as well as to various microorganisms for the synthesis of polyamines and the methylation of macromolecules (Figure 1) [8,9,10]

  • A number of fundamental investigations have disclosed the differences between the metabolic pathways of mammals and those of lower microorganisms such as Escherichia coli, Staphylococcus aureus, Salmonella typhi, Enterococcus faecalis, Mycobacterium tuberculosis, among others

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Summary

Introduction

During the last few years, physicians have been faced with little solutions to care bacterial infections and in particular those due to the advent of resistant bacteria such as MRSA (methicillin-resistant Staphylococcus aureus) [1,2,3]. A number of fundamental investigations have disclosed the differences between the metabolic pathways of mammals and those of lower microorganisms such as Escherichia coli, Staphylococcus aureus, Salmonella typhi, Enterococcus faecalis, Mycobacterium tuberculosis, among others. Some nucleoside analogues of MTA, either naturally derived or fully synthetic, acting as inhibitors of MTA/AdoHcy nucleosidase, have been discovered (Figure 2) [13,14,15]. Maining attached to the ribose moiety, depriving the cell of the necessary MTR (Figures 1 and 4)

Chemistry
Biology
Bioassays
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