Towards smart biocide-free anti-biofilm strategies: Click-based synthesis of cinnamide analogues as anti-biofilm compounds against marine bacteria

C Sall; M Ayé; O Bottzeck; A Praud; Y Blache

doi:10.1016/j.bmcl.2017.11.039

Towards smart biocide-free anti-biofilm strategies: Click-based synthesis of cinnamide analogues as anti-biofilm compounds against marine bacteria

Bioorg Med Chem Lett. 2018 Jan 15;28(2):155-159. doi: 10.1016/j.bmcl.2017.11.039. Epub 2017 Nov 24.

Authors

C Sall¹, M Ayé², O Bottzeck², A Praud², Y Blache³

Affiliations

¹ Laboratoire de chimie, UFR des Sciences de la Santé, Université de Thiès, BP 967 Thiès, Senegal.
² Laboratoire MAPIEM, Seatech Ecole d'ingénieurs, université de Toulon, CS 60584 Toulon Cedex 9, France.
³ Laboratoire MAPIEM, Seatech Ecole d'ingénieurs, université de Toulon, CS 60584 Toulon Cedex 9, France. Electronic address: [email protected].

PMID: 29198862
DOI: 10.1016/j.bmcl.2017.11.039

Abstract

A set of triazole-based analogues of N-coumaroyltyramine was designed to discover potential leads that may help in the control of bacterial biofilms. the most potent compounds act as inhibitors of biofilm development with EC50 closed to ampicillin (EC50 = 11 μM) without toxic effect on bacterial growth even at high concentrations(100 μM).

Keywords: 1,3 Cycloadditions; Anti-biofilm; Bacteria; Click chemistry; Triazole.

MeSH terms

Anti-Bacterial Agents / chemical synthesis
Anti-Bacterial Agents / chemistry
Anti-Bacterial Agents / pharmacology*
Biofilms / drug effects*
Coumaric Acids / chemical synthesis
Coumaric Acids / chemistry
Coumaric Acids / pharmacology*
Dose-Response Relationship, Drug
Microbial Sensitivity Tests
Molecular Structure
Paracoccus / drug effects*
Paracoccus / growth & development
Pseudoalteromonas / drug effects*
Pseudoalteromonas / growth & development
Structure-Activity Relationship

Substances

Anti-Bacterial Agents
Coumaric Acids