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J Org Chem
; 85(11): 7468-7475, 2020 06 05.
Artigo
em Inglês
| MEDLINE
| ID: mdl-32425046
RESUMO
Intracellular pathogens can thrive within mammalian cells and are inaccessible to many antimicrobial agents. Herein, we present a facile method of enhancing the cell penetrating and antibacterial properties of cationic amphiphilic polyproline helices (CAPHs) with modifications to the hydrophobic moiety at the N-terminus. These altered CAPHs display superior cell penetration within macrophage cells, and in some cases, minimal cytotoxicity. Furthermore, one CAPH, Pentyl-P14 exhibited excellent antibacterial activity against multiple strains of pathogenic bacteria and promoted the clearance of intracellular Shigella within macrophages.
Assuntos
Antibacterianos , Peptídeos , Animais , Antibacterianos/farmacologia , Bactérias , Cátions , Testes de Sensibilidade Microbiana , Peptídeos/farmacologia , Estrutura Secundária de Proteína
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