A Novel Derivative of Thioridazine Shows Low Toxicity and Efficient Activity against Gram-Positive Pathogens.
Gram-positive pathogens
novel antimicrobial compound
thioridazine
Journal
Antibiotics (Basel, Switzerland)
ISSN: 2079-6382
Titre abrégé: Antibiotics (Basel)
Pays: Switzerland
ID NLM: 101637404
Informations de publication
Date de publication:
15 Jun 2020
15 Jun 2020
Historique:
received:
06
05
2020
revised:
11
06
2020
accepted:
13
06
2020
entrez:
19
6
2020
pubmed:
19
6
2020
medline:
19
6
2020
Statut:
epublish
Résumé
Thioridazine hydrochloride (HCl) has been suggested as a promising antimicrobial helper compound for the treatment of infections with antimicrobial-resistant bacteria. Unfortunately, the therapeutic concentration of thioridazine HCl is generally higher than what can be tolerated clinically, in part due to its toxic side effects on the central nervous system. Therefore, we aimed to synthesize a less toxic thioridazine derivative that would still retain its properties as a helper compound. This resulted in a compound designated 1-methyl-2-(2-(2-(methylthio)-10H-phenothiazin-10-yl)ethyl)-1-pentylpiperidin-1-ium bromide (abbreviated T5), which exhibited low blood-brain barrier permeability. The lowest minimal inhibitory concentration (MIC) against
Identifiants
pubmed: 32549350
pii: antibiotics9060327
doi: 10.3390/antibiotics9060327
pmc: PMC7344759
pii:
doi:
Types de publication
Journal Article
Langues
eng
Subventions
Organisme : Danish Council of Independent Research
ID : 4184-00512
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