Structure-activity relationship analyses of fusidic acid derivatives highlight crucial role of the C-21 carboxylic acid moiety to its anti-mycobacterial activity.
Anti-mycobacterial activity
Bioisosteres
Cytotoxicity
Fusidic acid
Journal
Bioorganic & medicinal chemistry
ISSN: 1464-3391
Titre abrégé: Bioorg Med Chem
Pays: England
ID NLM: 9413298
Informations de publication
Date de publication:
01 07 2020
01 07 2020
Historique:
received:
12
03
2020
accepted:
22
04
2020
pubmed:
5
5
2020
medline:
24
3
2021
entrez:
5
5
2020
Statut:
ppublish
Résumé
Fusidic acid (FA) is a potent congener of the fusidane triterpenoid class of antibiotics. Structure-activity relationship (SAR) studies suggest the chemical structure of FA is optimal for its antibacterial activity. SAR studies from our group within the context of a drug repositioning approach in tuberculosis (TB) suggest that, as with its antibacterial activity, the C-21 carboxylic acid group is indispensable for its anti-mycobacterial activity. Further studies have led to the identification of 16-deacetoxy-16β-ethoxyfusidic acid (58), an analog which exhibited comparable activity to FA with an in vitro MIC
Identifiants
pubmed: 32362386
pii: S0968-0896(20)30356-4
doi: 10.1016/j.bmc.2020.115530
pii:
doi:
Substances chimiques
Anti-Bacterial Agents
0
Fusidic Acid
59XE10C19C
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
115530Informations de copyright
Copyright © 2020 Elsevier Ltd. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of Competing Interest The authors declared that there is no conflict of interest.