CAS: 528851-31-2; 7-((2-Aminoethyl)Amino)-1-Cyclopropyl-6-Fluoro-4-Oxo-1,4-Dihydroquinoline-3-Carboxylic Acid Hydrochloride

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7-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid ethylenediamine 1-cyclopropyl-6,7-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid

📜1-环丙基-6,7-二氟-1,4-二氢-4-氧喹啉-3-羧酸置于吡啶,盐酸体系中,用 1,4-二氧六环 作为反应溶剂,化学反应 16.0H,反应生成 去乙烯基环丙沙星盐酸盐
参考文献:Identification Of A Potent Small-Molecule Inhibitor Of Bacterial Dna Repair That Potentiates Quinolone Antibiotic Activity In Methicillin-Resistant Staphylococcus Aureus
标题:Identification Of A Potent Small-Molecule Inhibitor Of Bacterial Dna Repair That Potentiates Quinolone Antibiotic Activity In Methicillin-Resistant Staphylococcus Aureus
摘要:The Global Emergence Of Antibiotic Resistance Is One Of The Most Serious Challenges Facing Modern Medicine. There Is An Urgent Need For Validation Of New Drug Targets And The Development Of Small Molecules With Novel Mechanisms Of Action. We Therefore Sought To Inhibit Bacterial Dna Repair Mediated By The Addab/recbcd Protein Complexes As A Means To Sensitize Bacteria To Dna Damage Caused By The Host Immune System Or Quinolone Antibiotics. A Rational,Hypothesis-Driven Compound Optimization Identified Imp-1700 As A Cell-Active,Nanomolar Potency Compound. Imp-1700 Sensitized Multidrug-Resistant Staphylococcus Aureus To The Fluoroquinolone Antibiotic Ciprofloxacin,Where Resistance Results From A Point Mutation In The Fluoroquinolone Target,Dna Gyrase. Cellular Reporter Assays Indicated Imp-1700 Inhibited The Bacterial Sos-Response To Dna Damage,And Compoundfunctionalized Sepharose Successfully Pulled-Down The Addab Repair Complex. This Work Provides Validation Of Bacterial Dna Repair As A Novel Therapeutic Target And Delivers Imp-1700 As A Tool Molecule And Starting Point For Therapeutic Development To Address The Pressing Challenge Of Antibiotic Resistance.
DOI:10.1016/j.Bmc.2019.06.025