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RSS FeedsMolecules, Vol. 23, Pages 2868: Analogues of Muraymycin Nucleoside Antibiotics with Epimeric Uridine-Derived Core Structures (Molecules)

 
 

4 november 2018 13:02:54

 
Molecules, Vol. 23, Pages 2868: Analogues of Muraymycin Nucleoside Antibiotics with Epimeric Uridine-Derived Core Structures (Molecules)
 




Nucleoside analogues have found widespread application as antiviral and antitumor agents, but not yet as antibacterials. Naturally occurring uridine-derived ‘nucleoside antibiotics’ target the bacterial membrane protein MraY, an enzyme involved in peptidoglycan biosynthesis and a promising target for the development of novel antibacterial agents. Muraymycins represent a nucleoside-peptide subgroup of such MraY-inhibiting natural products. As part of detailed structure-activity relationship (SAR) studies on muraymycins and their analogues, we now report novel insights into the effects of stereochemical variations in the nucleoside core structure. Using a simplified version of the muraymycin scaffold, it was shown that some formal inversions of stereochemistry led to about one order of magnitude loss in inhibitory potency towards the target enzyme MraY. In contrast, epimers of the core motif with retained inhibitory activity were also identified. These 5′,6′-anti-configured analogues might serve as novel chemically tractable variations of the muraymycin scaffold for the future development of uridine-derived drug candidates.


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73 viewsCategory: Biochemistry, Chemistry, Molecular Biology
 
Molecules, Vol. 23, Pages 2869: Influence of Ligand Functionalization of UiO-66-Based Metal-Organic Frameworks When Used as Sorbents in Dispersive Solid-Phase Analytical Microextraction for Different Aqueous Organic Pollutants (Molecules)
Molecules, Vol. 23, Pages 2867: Synthesis of Acridines through Alkyne Addition to Diarylamines (Molecules)
 
 
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