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Investigation of Naphthyl–Polyamine Conjugates as Antimicrobials and Antibiotic Enhancers
- Source :
- Antibiotics, Vol 12, Iss 6, p 1014 (2023)
- Publication Year :
- 2023
- Publisher :
- MDPI AG, 2023.
-
Abstract
- As part of our search for new antimicrobials and antibiotic enhancers, a series of naphthyl- and biphenyl-substituted polyamine conjugates have been synthesized. The structurally-diverse library of compounds incorporated variation in the capping end groups and in the length of the polyamine (PA) core. Longer chain (PA-3-12-3) variants containing both 1-naphthyl and 2-naphthyl capping groups exhibited more pronounced intrinsic antimicrobial properties against methicillin-resistant Staphylococcus aureus (MRSA) (MIC ≤ 0.29 µM) and the fungus Cryptococcus neoformans (MIC ≤ 0.29 µM). Closer mechanistic study of one of these analogues, 20f, identified it as a bactericide. In contrast to previously reported diarylacyl-substituted polyamines, several examples in the current set were able to enhance the antibiotic action of doxycycline and/or erythromycin towards the Gram-negative bacteria Pseudomonas aeruginosa and Escherichia coli. Two analogues (19a and 20c) were of note, exhibiting greater than 32-fold enhancement in activity. This latter result suggests that α,ω-disubstituted polyamines bearing 1-naphthyl- and 2-naphthyl-capping groups are worthy of further investigation and optimization as non-toxic antibiotic enhancers.
Details
- Language :
- English
- ISSN :
- 20796382
- Volume :
- 12
- Issue :
- 6
- Database :
- Directory of Open Access Journals
- Journal :
- Antibiotics
- Publication Type :
- Academic Journal
- Accession number :
- edsdoj.9ac8a95b359490d9a748abe85c237c6
- Document Type :
- article
- Full Text :
- https://doi.org/10.3390/antibiotics12061014