Synthesis and antimicrobial activity of small cationic amphipathic aminobenzamide marine natural product mimics and evaluation of relevance against clinical isolates including ESBL–CARBA producing multi-resistant bacteria. Issue 22 (15th November 2016)

• Record Type: Journal Article
• Authors: Igumnova, Elizaveta M.; Mishchenko, Ekaterina; Haug, Tor; Blencke, Hans-Matti; Sollid, Johanna U. Ericson; Fredheim, Elizabeth G. Aarag; Lauksund, Silje; Stensvåg, Klara; Strøm, Morten B.
• Is Part Of: Bioorganic & medicinal chemistry. Volume 24:Issue 22(2016)
• Page Start: 5884
• Page End: 5894
• Publication Date: 2016-11-15
• Subjects: ESBL–CARBA -- Aminobenzamides -- Antibacterial -- Antimicrobial -- Marine natural product mimics -- Multi-resistant bacteria -- Peptidomimetics; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2016.09.046
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: Abstract: A library of small aminobenzamide derivatives was synthesised to explore a cationic amphipathic motif found in marine natural antimicrobials. The most potent compoundE23 displayed minimal inhibitory concentrations (MICs) of 0.5–2 μg/ml against several Gram-positive bacterial strains, including methicillin resistant Staphylococcus epidermidis (MRSE) . E23 was also potent against 275 clinical isolates including Staphylococcus aureus, Enterococcus spp ., Escherichia coli, Pseudomonas aeruginosa, and Klebsiella pneumoniae, as well as methicillin-resistant S. aureus (MRSA), vancomycin-resistant enterococci (VRE), and ESBL–CARBA producing multi-resistant Gram-negative bacteria. The study demonstrates how structural motifs found in marine natural antimicrobials can be a valuable source for making novel antimicrobial lead-compounds .