Abstract
A structure-activity relationship (SAR) for the oxadiazole class of antibacterials was evaluated by syntheses of 72 analogs and determination of the minimal-inhibitory concentrations (MICs) against the ESKAPE panel of bacteria. Selected compounds were further evaluated for in vitro toxicity, plasma protein binding, pharmacokinetics (PK), and a mouse model of methicillin-resistant Staphylococcus aureus (MRSA) infection. Oxadiazole 72c shows potent in vitro antibacterial activity, exhibits low clearance, a high volume of distribution, and 41% oral bioavailability, and shows efficacy in mouse models of MRSA infection.
Highlights
With a view to explore the structural space of this class of they saved millions of lives in treatment of infections, they have antibiotics, we recently reported a structure-activity made possible other medical interventions such as surgery, relationship (SAR) of the oxadiazoles against S. aureus[5] with a dialysis, and organ transplantation
26 antibiotics has contributed to the increase in life expectancy in the United States from 59.7 years in 1930 to 78.8 years in 2010.1 Notwithstanding, emergence of resistance to any antibiotic is chloropyrazole, or 5-indole substitutions were generally favored at this position (1, 2, and 4–8; Figure 1)
Staphylococcus aureus and Enterococci pose the biggest infected mice comparable to results obtained with linezolid, the threat.[2]
Summary
Peng†, Yuanyuan Qian†, Takao Yamaguchi†, Sebastian A. O’Daniel†, Erika Leemans†, Elena Lastochkin†, Wei Song†, Valerie A. KEYWORDS antibacterials, oxadiazoles, penicillin-binding proteins, structure-activity relationship
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