CAS: 62124-77-0; Ethyl 3-(2-Pyrazinyl)-3-Oxopropanoate

相似化合物

1617540-00-7 62124-83-8 75399-07-4

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CAS号141-78-6 乙酸乙酯 | CAS号6924-68-1 吡嗪-2-甲酸乙酯 | CAS号19847-10-0 2-吡嗪羰酰氯 | CAS号105-53-3 丙二酸二乙酯 | CAS号6164-79-0 2-吡嗪羧酸甲酯 | CAS号22047-25-2 2-乙酰基吡嗪 | CAS号105-58-8 碳酸二乙酯

📜2-甲酸吡嗪,丙二酸单乙酯置于n,N'-羰基二咪唑,甲基溴化镁体系中,用 四氢呋喃,乙醚,水 作为反应溶剂,化学反应 2.0H,以82%的收率获得产物3-(2-吡嗪基)-3-氧代丙酸乙酯
参考文献:Optimization Of Pyrrolamide Topoisomerase Ii Inhibitors Toward Identification Of An Antibacterial Clinical Candidate (Azd5099)
标题:Optimization Of Pyrrolamide Topoisomerase Ii Inhibitors Toward Identification Of An Antibacterial Clinical Candidate (Azd5099)
摘要:Azd5099 (Compound 63) Is An Antibacterial Agent That Entered Phase 1 Clinical Trials Targeting Infections Caused By Gram-Positive And Fastidious Gram-Negative Bacteria. It Was Derived From Previously Reported Pyrrolamide Antibacterials And A Fragment-Based Approach Targeting The Atp Binding Site Of Bacterial Type Ii Topoisomerases. The Program Described Herein Varied A 3-Piperidine Substituent And Incorporated 4-Thiazole Substituents That Form A Seven-Membered Ring Intramolecular Hydrogen Bond With A 5-Position Carboxylic Acid. Improved Antibacterial Activity And Lower In Vivo Clearances Were Achieved. The Lower Clearances Were Attributed,In Part,To Reduced Recognition By The Multidrug Resistant Transporter Mrp2. Compound 63 Showed Notable Efficacy In A Mouse Neutropenic Staphylococcus Aureus Infection Model. Resistance Frequency Versus The Drug Was Low,And Reports Of Clinical Resistance Due To Alteration Of The Target Are Few. Hence,63 Could Offer A Novel Treatment For Serious Issues Of Resistance To Currently Used Antibacterials.
DOI:10.1021/jm500462X