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Molecules 2018, 23(7), 1513;

A Novel Class of Cationic and Non-Peptidic Small Molecules as Hits for the Development of Antimicrobial Agents

Instituto de Química Médica, Consejo Superior de Investigaciones Científicas (IQM, CSIC), Juan de la Cierva 3, 28006 Madrid, Spain
Laboratorio de Patógenos Bacterianos Intracelulares, Centro Nacional de Biotecnología, Consejo Superior de Investigaciones Científicas (CNB, CSIC), Darwin 3, 28049 Madrid, Spain
Natac Biotech S.L., Parque Científico de Madrid, Campus de Cantoblanco, 28049 Madrid, Spain
These authors contributed equally to this work.
Current address: Agencia Española de Medicamentos y productos Sanitarios, Campezo 1, Edificio 8, 28022 Madrid, Spain.
Current address: Novartis Farmacéutica S.A. Gran Vía de les Corts Catalanes, 764, 08013 Barcelona, Spain.
Authors to whom correspondence should be addressed.
Academic Editor: Jóhannes Reynisson FRSC
Received: 6 June 2018 / Revised: 19 June 2018 / Accepted: 20 June 2018 / Published: 22 June 2018
(This article belongs to the Special Issue Hit Generation and Verification for Novel Lead Compounds)
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Cationic and non-peptide small molecules containing a total of six positive charges arranged on one side and a long aliphatic tail on the other have been synthesized and tested against Gram-positive and Gram-negative bacteria. The positive charges have been contributed by two aminophenol residues. These molecules have showed remarkable antimicrobial activity against Gram-positive bacteria including multidrug-resistant strains. Our structure–activity relationship studies demonstrated the importance of the length and flexibility of the hydrophobic tail for the antimicrobial activity. Importantly, these compounds are non-toxic to eukaryotic cells at the concentration affecting growth in bacteria, reflecting an acceptable margin of safety. The small size and easy synthetic accessibility of our molecules can be of interest for the further development of novel antimicrobials against Gram-positive bacterial pathogens, including multidrug-resistant strains. View Full-Text
Keywords: antimicrobial agents; antibiotic resistance; antimicrobial peptides antimicrobial agents; antibiotic resistance; antimicrobial peptides

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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 (CC BY 4.0).

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Jiménez, A.; García, P.; de la Puente, S.; Madrona, A.; Camarasa, M.J.; Pérez-Pérez, M.-J.; Quintela, J.-C.; García-del Portillo, F.; San-Félix, A. A Novel Class of Cationic and Non-Peptidic Small Molecules as Hits for the Development of Antimicrobial Agents. Molecules 2018, 23, 1513.

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