1047981-31-6
Chemical Structure
AFN-1252 tosylate
Synonym(s): API-1252 tosylate; Debio 1452 tosylate
- CAS No.: 1047981-31-6
- Formula:C29H29N3O6S
- Molecular Weight:547.62
IUPAC Name: (E)-N-methyl-N-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-1,5,6,7-tetrahydro-1,8-naphthyridin-3-yl)acrylamide 4-methylbenzenesulfonate
InChIKey: NHTYVWVPSCBFQW-HCUGZAAXSA-N
SMILES: O=S(O)(C1=CC=C(C=C1)C)=O.CC2=C(CN(C)C(/C=C/C(C=C3CC4)=CNC3=NC4=O)=O)OC5=CC=CC=C25
Biological Activity: AFN-1252 (API-1252) tosylate is an orally active and selective inhibitor of FabI, an essential enzyme in fatty acid biosynthesis in Staphylococcus spp. AFN-1252 tosylate exhibits exquisite and highly selective activity against Staphylococcus spp. AFN-1252 tosylate exhibits typical MIC90 values of 0.015 μg/ml against diverse clinical isolates of S. aureus. AFN-1252 tosylate is efficacious in a mouse model of septicemia providing 100% protection from an otherwise lethal peritoneal infection of S. aureus Smith[1][2].
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AFN-1252 tosylate | AFN-1252 (API-1252) tosylate is an orally active and selective inhibitor of FabI, an essential enzyme in fatty acid biosynthesis in Staphylococcus spp. AFN-1252 tosylate exhibits exquisite and highly selective activity against Staphylococcus spp. AFN-1252 tosylate exhibits typical MIC90 values of 0.015 μg/ml against diverse clinical isolates of S. aureus. AFN-1252 tosylate is efficacious in a mouse model of septicemia providing 100% protection from an otherwise lethal peritoneal infection of S. aureus Smith. | |||||||||||||||||||||
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References
- [1]. Nachum Kaplan, et al. In vitro activity (MICs and rate of kill) of AFN-1252, a novel FabI inhibitor, in the presence of serum and in combination with other antibiotics. J Chemother. 2013 Feb;25(1):18-25. [Content Brief]
- [2]. Nachum Kaplan,et al. Mode of action, in vitro activity, and in vivo efficacy of AFN-1252, a selective antistaphylococcal FabI inhibitor. Antimicrob Agents Chemother. 2012 Nov;56(11):5865-74. [Content Brief]
