📜三氟乙酰乙酸乙酯,3,5-二氯苯胺置于ppa体系中,化学反应生成 5,7-二氯-4-羟基-2-(三氟甲基)喹啉
参考文献:Structure−activity Relationships For A Series Of Quinoline-Based Compounds Active Against Replicating And Nonreplicating Mycobacterium Tuberculosis
标题:Structure−activity Relationships For A Series Of Quinoline-Based Compounds Active Against Replicating And Nonreplicating Mycobacterium Tuberculosis
摘要:Tuberculosis (Tb) Remains As A Global Pandemic That Is Aggravated By A Lack Of Health Care,The Spread Of Hiv,And The Emergence Of Multidrug-Resistant Tb (Mdr-Tb) And Extensively Drug-Resistant Tb (Xdr-Tb) Strains. New Anti-Tb Drugs Are Urgently Required To Shorten The Long 6-12 Month Treatment Regimen And To Battle Drug-Resistant Mtb Strains. We Have Identified Several Potent Quinoline-Based Anti-Tb Compounds,Bearing An Isoxazole Containing Side-Chain. The Most Potent Compounds,7G And 13,Exhibited Submicromolar Activity Against The Replicating Bacteria (R-Tb),With Minimum Inhibitory Concentrations (Mics) Of 0.77 And 0.95 Mu M,Respectively. In General,These Compounds Also Had Micromolar Activity Against The Nonreplicating Persistent Bacteria (Nrp-Tb) And Did Not Show Toxicity On Vero Cells Up To 128 Mu M Concentration. Compounds 7G And 13 Were Shown To Retain Their Anti-Tb Activity Against Rifampin,Isoniazid,And Streptomycin Resistant Mtb Strains. The Results Suggest That Quinoline-Isoxazole-Based Anti-Tb Compounds Are Promising Leads For New Tb Drug Development.
DOI:10.1021/jm900003C