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1.
Org Biomol Chem ; 19(44): 9624-9628, 2021 11 18.
Artigo em Inglês | MEDLINE | ID: mdl-34709282

RESUMO

Cyclodextrins have been employed as delivery agents for lipophilic anion transporters, which allow their incorporation into lipid bilayers without using an organic solvent or pre-incorporation.

2.
Eur J Med Chem ; 261: 115853, 2023 Dec 05.
Artigo em Inglês | MEDLINE | ID: mdl-37857144

RESUMO

Teixobactin is a cyclic undecadepsipeptide that has shown excellent potency against multidrug-resistant pathogens, such as methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococci (VRE). In this article, we present the design, synthesis, and antibacterial evaluations of 16 different teixobactin analogues. These simplified analogues contain commercially available hydrophobic, non-proteogenic amino acid residues instead of synthetically challenging expensive L-allo-enduracididine amino acid residue at position 10 together with different combinations of arginines at positions 3, 4 and 9. The new teixobactin analogues showed potent antibacterial activity against a broad panel of Gram-positive bacteria, including MRSA and VRE strains. Our work also presents the first demonstration of the potent antibiofilm activity of teixobactin analogoues against Staphylococcus species associated with serious chronic infections. Our results suggest that the use of hydrophobic, non-proteogenic amino acids at position 10 in combination with arginine at positions 3, 4 and 9 holds the key to synthesising a new generation of highly potent teixobactin analogues to tackle resistant bacterial infections and biofilms.


Assuntos
Staphylococcus aureus Resistente à Meticilina , Enterococos Resistentes à Vancomicina , Relação Estrutura-Atividade , Aminoácidos/farmacologia , Antibacterianos/química , Biofilmes , Testes de Sensibilidade Microbiana
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