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Cover Feature: Synthesis and Antibacterial Activity of New N ‐Alkylammonium and Carbonate‐Triazole Derivatives within Desosamine of 14‐ and 15‐Membered Lactone Macrolides (ChemMedChem 16/2020)
Author(s) -
Janas Anna,
Pecyna Paulina,
Gajecka Marzena,
Bartl Franz,
Przybylski Piotr
Publication year - 2020
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.202000578
Subject(s) - chemistry , stereochemistry , moiety , antibacterial activity , triazole , stacking , ribosomal rna , combinatorial chemistry , bacteria , biochemistry , biology , organic chemistry , genetics , gene
The Cover Feature shows one of promising 14‐membered lactone macrolide derivatives (bottom right) with antibacterial activity and decreased toxicity, for which the molecule has a crab‐like shape (bottom left), and is decorated with an unsaturated motif at one of the crab claws. These types of macrolide derivatives, due to an additionally armed crab claw e.g., desosamine linked with the unsaturated moiety of less bulkiness, are able to efficiently bind to the ribosomal tunnel of bacteria (top). Blocking the ribosomal tunnel via π–π stacking and H‐bonds with nucleotides of peptidyl transferase (top) disturbs the translation process and contributes to the antibacterial potency against S. pneumoniae and S. pyogenes strains. Cover design by Przybylski & Janas. More information can be found in the Full Paper by Piotr Przybylski et al.