AFN-1252 is an inhibitor of staphylococcal enoyl-acyl carrier protein reductase (FabI; Ki = 12.8 nM), an enzyme that activates bacterial fatty acid biosynthesis.
CAS：620175-39-5
分子式：C22H21N3O3
分子量：375.4
纯度：98%
存储：Store at -20°C

Background:

AFN-1252(Debio 1452) is a potent inhibitor of enoyl-acyl carrier protein reductase (FabI), inhibited all clinical isolates of Staphylococcus aureus and Staphylococcus epidermidis at concentrations of ≤0.12 μg/ml. IC50 value:Target: Antibiotic agentAFN-1252 was inactive (MIC90, >4 μg/ml) against clinical isolates of Streptococcus pneumoniae, beta-hemolytic streptococci, Enterococcus spp., Enterobacteriaceae, nonfermentative gram-negative bacilli, and Moraxella catarrhalis. These data support the continued development of AFN-1252 for the treatment of patients with resistant staphylococcal infections.

参考文献:
[1]. Karlowsky JA, et al. AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity. Antimicrob Agents Chemother. 2009 Aug;53(8):3544-8.
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[3]. Yao J, et al. Resistance to AFN-1252 arises from missense mutations in Staphylococcus aureus enoyl-acyl carrier protein reductase (FabI). J Biol Chem. 2013 Dec 20;288(51):36261-71.
[4]. Parsons JB, et al. Perturbation of Staphylococcus aureus gene expression by the enoyl-acyl carrier protein reductase inhibitor AFN-1252. Antimicrob Agents Chemother. 2013 May;57(5):2182-90.