Virtual Talk on: Rational design of balanced dual-targeting antibacterial compounds with limited resistance

Speaker: Prof. Lucija Peterlin Mašič, University of Ljubljana

Date: Tues, Oct 6, 2020 14:00-15:00 CET

Dial in via Zoom: https://zoom.us/j/98886770244

Abstract: Antibiotics that inhibit multiple bacterial targets offer a promising therapeutic strategy against resistance evolution, but developing such antibiotics is challenging. Here we demonstrate that a rational design of balanced multitargeting antibiotics is feasible by using a medicinal chemistry workflow. The resultant lead compounds belonging to a novel chemical class, almost equipotently inhibit bacterial DNA gyrase and topoisomerase IV complexes and interact with multiple evolutionary conserved amino acids in the ATP-binding pockets of their target proteins. Compounds are excellently potent against a broad range of gram-positive bacteria.