AFN-1252

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. It is selective for isolates of methicillin-susceptible and methicillin-resistant S. aureus (MIC90s = =0.008 µg/ml) over isolates of S. pneumoniae, beta-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.Formal Name: N-methyl-N-[(3-methyl-2E-benzofuranyl)methyl]-3-(5,6,7,8-tetrahydro-7-oxo-1,8-naphthyridin-3-yl)-2-propenamide. CAS Number: 620175-39-5. Synonyms: API-1252, Debio 1452. Molecular Formula: C22H21N3O3. Formula Weight: 375.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. lambdamax: 252, 286, 322 nm. SMILES: O=C1CCC2=CC(/C=C/C(N(CC3=C(C)C(C=CC=C4)=C4O3)C)=O)=CNC2=N1. InChi Code: InChI=1S/C22H21N3O3/c1-14-17-5-3-4-6-18(17)28-19(14)13-25(2)21(27)10-7-15-11-16-8-9-20(26)24-22(16)23-12-15/h3-7,10-12H,8-9,13H2,1-2H3,(H,23,24,26)/b10-7+. InChi Key: QXTWSUQCXCWEHF-JXMROGBWSA-N.