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Abstract

Design, Synthesis and Activity of New Polymyxins †

by
Francesc Rabanal
1,*,
Roser Segovia
1,
Aina Coll
1,
Judith Solé
1,
Maria Garcia-Subirats
1,
Angeles Manresa
2 and
Yolanda Cajal
3,4
1
Section of Organic Chemistry, Department of Inorganic and Organic Chemistry, Faculty of Chemistry, University of Barcelona, 08007 Barcelona, Spain
2
Laboratory of Microbiology, Faculty of Pharmacy, University of Barcelona, 08007 Barcelona, Spain
3
Department of Pharmacy, Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, 08028 Barcelona, Spain
4
Institute of Nanoscience and Nanotechnology (IN2UB), University of Barcelona, 08028 Barcelona, Spain
*
Author to whom correspondence should be addressed.
†
Presented at the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain, 8 September 2017.
Proceedings 2017, 1(6), 662; https://doi.org/10.3390/proceedings1060662
Published: 20 October 2017
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
Versions Notes
Antibiotic resistance is a daunting challenge for public health systems worldwide. A major goal to fight resistant bacteria involves the design, discovery and development of new antibiotics, particularly against multi-drug-resistant strains. Currently, there is renewed interest in polymyxins, an old class of antimicrobial cyclic lipopeptides, highly potent against therapeutically relevant Gram-negative bacteria. Polymyxins are now used as last resort antibiotics in hospitals because of their nephrotoxicity and neurotoxicity that requires careful monitoring of the patient. Our group has embarked on a project to design and develop new polymyxins devoid of toxicity problems using a versatile and chemically accessible scaffold structure [1,2]. Compounds show excellent activity against Gram-negative bacteria. Synergistic and antibiofilm activities have also been recently described in combination with imipenem [3]. Herein, the latest results of our recently designed polymyxin analogs will be presented.

Acknowledgments

The research was supported by the University of Barcelona, Fundació Bosch i Gimpera, Xarxa de Referència en Biotecnologia, 2016LLAVO0018 grant (Generalitat de Catalunya) and the European Institute of Innovation and Technology (EIT Health). The authors are members of the ENABLE (European Gram-negative Antibacterial Engine) consortium (IMI-ND4BB, http://www.imi.europa.eu/projects-results/project-factsheets/enable).

Author Contributions

RS, AC, MGS and JS performed research, AM and YC supervised research. FR directed the whole research and writing

Conflicts of Interest

The authors declare no conflict of interest

References

  1. Rabanal, F.; Grau-Campistany, A.; Vila-Farrés, X.; González-Linares, J.; Borras, J.M.; Vila, J.; Manresa, A.; Cajal, Y. A bioinspired peptide scaffold with high antibiotic activity and low in vivo toxicity Sci. Rep. 2015, 5, 10558. Available online: https://www.nature.com/articles/srep10558 (accessed on 10 October 2017).
  2. Rabanal, F.; Cajal, Y. Recent advances and perspectives in the design and development of polymyxins. Nat. Prod. Rep. 2017, 34, 886. [Google Scholar] [CrossRef] [PubMed]
  3. Rudilla, H.; Fusté, E.; Cajal, Y.; Rabanal, F.; Vinuesa, T.; Viñas, M. Synergistic antipseudomonal effects of synthetic peptide AMP38 and carbapenems. Molecules 2016, 21, 1223. Available online: https://www.mdpi.com/1420-3049/21/9/1223 (accessed on 10 October 2017). [CrossRef] [PubMed]
Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations.

Share and Cite

MDPI and ACS Style

Rabanal, F.; Segovia, R.; Coll, A.; Solé, J.; Garcia-Subirats, M.; Manresa, A.; Cajal, Y. Design, Synthesis and Activity of New Polymyxins. Proceedings 2017, 1, 662. https://doi.org/10.3390/proceedings1060662

AMA Style

Rabanal F, Segovia R, Coll A, Solé J, Garcia-Subirats M, Manresa A, Cajal Y. Design, Synthesis and Activity of New Polymyxins. Proceedings. 2017; 1(6):662. https://doi.org/10.3390/proceedings1060662

Chicago/Turabian Style

Rabanal, Francesc, Roser Segovia, Aina Coll, Judith Solé, Maria Garcia-Subirats, Angeles Manresa, and Yolanda Cajal. 2017. "Design, Synthesis and Activity of New Polymyxins" Proceedings 1, no. 6: 662. https://doi.org/10.3390/proceedings1060662

APA Style

Rabanal, F., Segovia, R., Coll, A., Solé, J., Garcia-Subirats, M., Manresa, A., & Cajal, Y. (2017). Design, Synthesis and Activity of New Polymyxins. Proceedings, 1(6), 662. https://doi.org/10.3390/proceedings1060662

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