Tuning the Anthranilamide Peptidomimetic Design to Selectively Target Planktonic Bacteria and Biofilm-Reference-Cited by-同舟云学术

Tuning the Anthranilamide Peptidomimetic Design to Selectively Target Planktonic Bacteria and Biofilm

Published:2023-03-15 Issue:3 Volume:12 Page:585
ISSN:2079-6382
Container-title:Antibiotics
language:en
Short-container-title:Antibiotics

Author:

Kuppusamy Rajesh¹²^ORCID,Yasir Muhammad²,Yu Tsz Tin¹^ORCID,Voli Florida³,Vittorio Orazio³⁴⁵^ORCID,Miller Michael J.⁶,Lewis Peter⁷^ORCID,Black David StC¹^ORCID,Willcox Mark²^ORCID,Kumar Naresh¹^ORCID

Affiliation:

1. School of Chemistry, The University of New South Wales (UNSW), Sydney, NSW 2052, Australia

2. School of Optometry and Vision Science, The University of New South Wales (UNSW), Sydney, NSW 2052, Australia

3. Children’s Cancer Institute, Lowy Cancer Research Centre, University of New South Wales, Sydney, NSW 2052, Australia

4. School of Clinical Medicine, University of New South Wales, Sydney, NSW 2052, Australia

5. ARC Centre of Excellence in Convergent Bio-Nano Science and Technology, University of New South Wales, Sydney, NSW 2052, Australia

6. School of Environmental and Life Sciences, College of Engineering, Science and Environment, The University of Newcastle, Newcastle, NSW 2308, Australia

7. Hunter Biological Solutions Pty Ltd., Newcastle, NSW 2310, Australia

Abstract

There is a pressing need to develop new antimicrobials to help combat the increase in antibiotic resistance that is occurring worldwide. In the current research, short amphiphilic antibacterial and antibiofilm agents were produced by tuning the hydrophobic and cationic groups of anthranilamide peptidomimetics. The attachment of a lysine cationic group at the tail position increased activity against E. coli by >16-fold (from >125 μM to 15.6 μM) and greatly reduced cytotoxicity against mammalian cells (from ≤20 μM to ≥150 μM). These compounds showed significant disruption of preformed biofilms of S. aureus at micromolar concentrations.

Funder

Australian Research Council Discovery project

National Health and Medical Research Ideas grant

Publisher

MDPI AG

Subject

Pharmacology (medical),Infectious Diseases,Microbiology (medical),General Pharmacology, Toxicology and Pharmaceutics,Biochemistry,Microbiology

Link

https://www.mdpi.com/2079-6382/12/3/585/pdf

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