2245691-60-3
2245691-60-3
Chemical Structure
Type II topoisomerase inhibitor 1
- CAS No.: 2245691-60-3
- Formula:C18H15N3O4
- Molecular Weight:337.33
IUPAC Name: 4-(8-(methylamino)-2-oxo-1,2-dihydroquinoline-3-carboxamido)benzoic acid
InChIKey: VUXYPRAXFABKBH-UHFFFAOYSA-N
SMILES: CNC1=CC=CC2=C1NC(C(C(NC3=CC=C(C=C3)C(O)=O)=O)=C2)=O
Biological Activity: Type II topoisomerase inhibitor 1 is a potent and selective E. coli DNA gyrase inhibitor (IC50: 1.7 nM), and forms hydrogen bonds with Asp73 residue. Type II topoisomerase inhibitor 1 inhibits topoisomerase IV activity (IC50: 0.98 μM). Type II topoisomerase inhibitor 1 can be used in the research of antibacterial area[1][2].
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Type II topoisomerase inhibitor 1 | Type II topoisomerase inhibitor 1 is a potent and selective E. coli DNA gyrase inhibitor (IC50: 1.7 nM), and forms hydrogen bonds with Asp73 residue. Type II topoisomerase inhibitor 1 inhibits topoisomerase IV activity (IC50: 0.98 μM). Type II topoisomerase inhibitor 1 can be used in the research of antibacterial area. | |||||||||||||||||||||
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References
- [1]. Fumihito Ushiyama, et al. Lead Identification of 8-(Methylamino)-2-oxo-1,2-dihydroquinoline Derivatives as DNA Gyrase Inhibitors: Hit-to-Lead Generation Involving Thermodynamic Evaluation. ACS Omega. 2020 Apr 24;5(17):10145-10159. [Content Brief]
- [2]. Fumihito Ushiyama, et al. Lead optimization of 8-(methylamino)-2-oxo-1,2-dihydroquinolines as bacterial type II topoisomerase inhibitors. Bioorg Med Chem. 2020 Nov 15;28(22):115776. [Content Brief]
