Synthesis of Fusidic Acid Derivatives Yields a Potent Antibiotic with an Improved Resistance Profile.
EF-G inhibitor
antibiotics
fusidic acid analogues
in vivo efficacy
resistance profile
Journal
ACS infectious diseases
ISSN: 2373-8227
Titre abrégé: ACS Infect Dis
Pays: United States
ID NLM: 101654580
Informations de publication
Date de publication:
12 02 2021
12 02 2021
Historique:
pubmed:
2
2
2021
medline:
24
6
2021
entrez:
1
2
2021
Statut:
ppublish
Résumé
Fusidic acid (FA) is a potent steroidal antibiotic that has been used in Europe for more than 60 years to treat a variety of infections caused by Gram-positive pathogens. Despite its clinical success, FA requires significantly elevated dosing (3 g on the first day, 1.2 g on subsequent days) to minimize resistance, as FA displays a high resistance frequency, and a large shift in minimum inhibitory concentration is observed for resistant bacteria. Despite efforts to improve on these aspects, all previously constructed derivatives of FA have worse antibacterial activity against Gram-positive bacteria than the parent natural product. Here, we report the creation of a novel FA analogue that has equivalent potency against clinical isolates of
Identifiants
pubmed: 33522241
doi: 10.1021/acsinfecdis.0c00869
pmc: PMC8713577
mid: NIHMS1764349
doi:
Substances chimiques
Anti-Bacterial Agents
0
Fusidic Acid
59XE10C19C
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Research Support, U.S. Gov't, Non-P.H.S.
Langues
eng
Sous-ensembles de citation
IM
Pagination
493-505Subventions
Organisme : NIAID NIH HHS
ID : R01 AI136773
Pays : United States
Organisme : NIGMS NIH HHS
ID : T32 GM136629
Pays : United States
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