620175-39-5

620175-39-5 structure

Name: AFN-1252
Chemical Name: (E)-N-methyl-N-[(3-methyl-1-benzofuran-2-yl)methyl]-3-(7-oxo-6,8-dihydro-5H-1,8-naphthyridin-3-yl)prop-2-enamide
CAS Number: 620175-39-5
Molecular Formula: C₂₂H₂₁N₃O₃
Molecular Weight: 375.42000
Catalog: Signaling Pathways Anti-infection Bacterial
Create Date: 2017-01-08 12:55:05
Modify Date: 2025-08-29 17:14:53
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.

Name	(E)-N-methyl-N-[(3-methyl-1-benzofuran-2-yl)methyl]-3-(7-oxo-6,8-dihydro-5H-1,8-naphthyridin-3-yl)prop-2-enamide
Synonyms	afn-1252 unii-t3o718ikkm api-1252

Description	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.
Related Catalog	Signaling Pathways >> Anti-infection >> Bacterial Research Areas >> Infection
References	[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. [2]. Narasimha Rao K, et al. AFN-1252 is a potent inhibitor of enoyl-ACP reductase from Burkholderia pseudomallei-Crystal structure, mode of action, and biological activity. Protein Sci. 2015 May;24(5):832-40. [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.