AFN-1252

AFN-1252 is an inhibitor of staphylococcal enoyl-acyl carrier protein reductase (FabI; K_i = 12.8 nM), an enzyme that activates bacterial fatty acid biosynthesis.^1,2,3 It is selective for isolates of methicillin-susceptible and methicillin-resistant S. aureus (MIC₉₀s = ≤0.008 μg/ml) over isolates of S. pneumoniae, β-hemolytic streptococci, Enterococcus, Enterobacteriaceae, non-fermentative Gram-negative bacilli, and M. catarrhalis (MIC₉₀s = >4 μg/ml). In vivo, AFN-1252 increases survival in a murine acute lethal septicemia model, showing 100% survival when administered at a single oral dose of 1 mg/kg.¹

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1. Kaplan, N.O., Albert, M., Awrey, D.E., et al. Mode of action, in vitro activity, and in vivo efficacy of AFN-1252, a selective antistaphylococcal FabI inhibitor. Antimicrob. Agents Chemother. 56(11), 5865-5874 (2012).

2. Parsons, J.B., Frank, M.W., Subramanian, S., et al. Metabolic basis for the differential susceptibility of Gram-positive pathogens to fatty acid synthesis inhibitors. Proc. Natl. Acad. Sci. USA 108(37), 15378-15383 (2011).

3. Karlowsky, J.A., Kaplan, N.O., Hafkin, B., et al. AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity. Antimicrob. Agents Chemother. 53(8), 3544-3548 (2009).