Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Antimicrobial Properties of New Polyamines Conjugated with Oxygen Containing Aromatic Functional Groups

Mario Inclán
* ORCID logo ,
Neus Torres Hernández
ORCID logo ,
Alejandro Martínez Serra
ORCID logo ,
Gonzalo Torrijos Jabón
ORCID logo ,
Salvador Blasco
ORCID logo ,
Cecilia Andreu
* ,
Marcel·lí Del Olmo
,
Beatriz Jávega
ORCID logo ,
Enrique O'Connor
,
Enrique García-España
* ORCID logo
Version 1 : Received: 12 October 2023 / Approved: 13 October 2023 / Online: 16 October 2023 (05:36:24 CEST)

A peer-reviewed article of this Preprint also exists.

Inclán, M.; Torres Hernández, N.; Martínez Serra, A.; Torrijos Jabón, G.; Blasco, S.; Andreu, C.; del Olmo, M.L.; Jávega, B.; O’Connor, J.-E.; García-España, E. Antimicrobial Properties of New Polyamines Conjugated with Oxygen-Containing Aromatic Functional Groups. Molecules 2023, 28, 7678. Inclán, M.; Torres Hernández, N.; Martínez Serra, A.; Torrijos Jabón, G.; Blasco, S.; Andreu, C.; del Olmo, M.L.; Jávega, B.; O’Connor, J.-E.; García-España, E. Antimicrobial Properties of New Polyamines Conjugated with Oxygen-Containing Aromatic Functional Groups. Molecules 2023, 28, 7678.

Abstract

Antibiotic resistance is now a first-order health problem, which makes the development of new families of antimicrobials an imperative. These compounds should ideally be inexpensive, readily available, highly active and non-toxic. Here we present the results on the antimicrobial activity of a series of natural and synthetic polyamines with different architectures (linear, tripodal and macrocyclic) and their derivatives containing the oxygen containing aromatic functional groups 1,3-benzodioxol, ortho/para phenol or 2,3-dihydrobenzofuran. The new compounds were prepared through a non-expensive process and their activity was tested against selected strains of yeast, gram-positive and gram-negative bacteria. In all cases, the conjugated derivatives showed antimicrobial activity higher than the unsubstituted polyamines. Several factors, such as the overall charge at physiological pH, the lipophilicity and the topology of the polyamine scaffold were relevant to their activity. The nature of the lipophilic moiety was also determinant on human cell toxicity. The lead compounds showed to be bactericidal and fungistatic, and they were synergic with the commercial antifungals fluconazole, cycloheximide and amphotericin B against the yeast strains tested.

Keywords

polyamine; antimicrobial; bacteria; yeast; synergy; bactericidal; fungistatic

Subject

Physical Sciences, Chemical Physics

Copyright: This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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