CAS: 100361-18-0; 7-Chloro-1-Cyclopropyl-6-Fluoro-1,4-Dihydro-4-Oxo-1,8-Naphthyridine-3-Carboxylic Acid

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96568-07-9 2606822-35-7 137118-01-5

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CAS号96568-07-9 1-环丙基-4-氧代-6-氟-... | CAS号99735-42-9 1-cyclopropyl-6... | CAS号96568-04-6 3-(2,6-二氯-5-氟-3... | CAS号122-51-0 原甲酸三乙酯 | CAS号765-30-0 环丙胺 | CAS号96568-07-9 1-环丙基-4-氧代-6-氟-... | CAS号113533-65-6 1-cyclopropyl-6... | CAS号122536-91-8 1-cyclopropyl-6...

3-环丙基氨基-2-(2,6-二氯-5-氟吡啶-3-羰基)丙烯酸酯置于potassium Phosphate,盐酸,溶剂黄146体系中,用 乙腈,水 用作溶剂,化学反应生成环丙基萘啶羧酸
参考文献:Novel Lead Generation Of An Anti-Tuberculosis Agent Active Against Non-Replicating Mycobacteria: Exploring Hybridization Of Pyrazinamide With Multiple Fragments
标题:Novel Lead Generation Of An Anti-Tuberculosis Agent Active Against Non-Replicating Mycobacteria: Exploring Hybridization Of Pyrazinamide With Multiple Fragments
摘要:The Key To Shortening Tuberculosis (Tb) Drug Regimen Lies In Eliminating The Reservoir Of Non-Replicating Persistent (Nrp) Mycobacterium Tuberculosis (Mtb). Pyrazinamide (Pza) Is The Only Known Drug Used As Part Of A Combination Therapy That Is Believed To Kill Nrp Mtb And Achieve Sterilization. Pza Is Active Only Under Low Ph Screening Conditions. Screening And Identification Of Nrp-Active Anti-Tb Compounds Are Severely Limited Because Compounds Are Usually Inactive Under Regular Assay Conditions. In An Effort To Design Novel Nrp-Active Anti-Tb Compounds,We Used Pyrazinamide As A Core And Hybridized It With The Fragments Derived From Marketed Drugs. One Of These Designs,Compound 8,Was A Hybrid With Fluoroquinolone. This Compound Exhibited > 10 Fold Improvement In Nrp Activity Under Low Ph Condition As Compared To Pyrazinamide And A Modest Activity (0.8 Log(10) Kill) Under Nutritionally Starved Nrp Condition. Furthermore,Compound 8 Was Active Against Fluoroquinolone-Resistant Strains And Did Not Show Any Activity In A Dna Supercoiling Assay (Gyrase Inhibition),Suggesting That Its Mechanism Of Action Is Not That Of The Parent Fluoroquinolone. These Results Provide A Novel Avenue In The Exploration Of New Chemotypes That Are Active Against Non-Replicating Mtb.
Doi:10.1007/s00044-015-1352-6

专利信息

专利号:RU-2120940-C1
优先权日:1994-06-16
标题:Derivatives of quinoline- or naphthyridine carboxylic acid and methods of their synthesis