Identification and characterization of a new antimicrobial chemical series

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Antibiotic resistance represents a major health problem for society. With the expanded use of antibiotics,**microorganisms have developed various mechanisms of resistance to overcome the cytotoxic effects of once**highly effective agents. Staphylococcus aureus (S. aureus) represents one such organism that has developed**rapid resistance to methicillin two years after its introduction into clinical settings. However,**methicillin-resistant S. aureus (MRSA) has started to show resistance to vancomycin, considered the standard**of care for the last decades. There is therefore an urgent need to identify novel therapeutics to counteract**resistant strains. The proposed project aims at identifying new chemical series that can overcome the antibiotic**resistance observed with Enterococci and MRSA. Starting from an initial proprietary compound, the physical**and chemical properties of the series will be investigated and enhanced to ensure high potency with good**solubility and pharmacokinetic properties. Structure activity relationship (SAR) studies will be performed**using in vitro assays and assess the minimal inhibitory concentration (MIC) and bactericidal activity of each**chemical series.