📜4,4,4-三氟-1-(2-菲基)-1,3-丁烷二酮置于盐酸,Platinum(Iv) Oxide,氢气,盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺体系中,用 四氢呋喃,乙醇,乙酸乙酯 作为反应溶剂,化学反应生成 2-氨基-N-[4-[5-(2-菲基)-3-(三氟甲基)-1H-吡唑-1-基]苯基]乙酰胺
参考文献:Development Of Novel Antibacterial Agents Against Methicillin-Resistant Staphylococcus Aureus
标题:Development Of Novel Antibacterial Agents Against Methicillin-Resistant Staphylococcus Aureus
摘要:Methicillin-Resistant Staphylococcus Aureus (Mrsa) Poses A Serious Threat To Public Health Because Of Its Resistance To Multiple Antibiotics Most Commonly Used To Treat Infection. In This Study,We Report The Unique Ability Of The Cyclooxygenase-2 (Cox-2) Inhibitor Celecoxib To Kill Staphylococcus Aureus And Mrsa With Modest Potency. We Hypothesize That The Anti-Staphylococcus Activity Of Celecoxib Could Be Pharmacologically Exploited To Develop Novel Anti-Mrsa Agents With A Distinct Mechanism. Examination Of An In-House,Celecoxib-Based Focused Compound Library In Conjunction With Structural Modifications Led To The Identification Of Compound 46 As The Lead Agent With High Antibacterial Potency Against A Panel Of Staphylococcus Pathogens And Different Strains Of Mrsa. Moreover,This Killing Effect Is Bacteria-Specific,As Human Cancer Cells Are Resistant To 46. In Addition,A Single Intraperitoneal Administration Of Compound 46 At 30 Mg/kg Improved The Survival Of Mrsa-Infected C57Bl/6 Mice. In Light Of Its High Potency In Eradicating Mrsa In Vitro And Its In Vivo Activity,Compound 46 And Its Analogues Warrant Continued Preclinical Development As A Potential Therapeutic Intervention Against Mrsa. (C) 2012 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmc.2012.06.018