CAS: 1225208-94-5; (6R,7R)-7-((Z)-2-(2-Aminothiazol-4-yl)-2-(((2-Carboxypropan-2-yl)Oxy)Imino)Acetamido)-3-((1-(2-(2-Chloro-3,4-Dihydroxybenzamido)Ethyl)Pyrrolidin-1-Ium-1-yl)Methyl)-8-Oxo-5-Thia-1-Azabicyclo[4.2.0]Oct-2-Ene-2-Carboxylate

📜2-氯-3,4-二甲氧基苯甲酸置于三溴化硼,Potassium Carbonate,甲基磺酰氯,三乙胺,Sodium Iodide,Sodium Hydroxide体系中,用 四氢呋喃,甲醇,二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,化学反应 14.33H,反应生成头孢地尔
参考文献:Cefiderocol (S-649266),A New Siderophore Cephalosporin Exhibiting Potent Activities Against Pseudomonas Aeruginosa And Other Gram-Negative Pathogens Including Multi-Drug Resistant Bacteria: Structure Activity Relationship
标题:Cefiderocol (S-649266),A New Siderophore Cephalosporin Exhibiting Potent Activities Against Pseudomonas Aeruginosa And Other Gram-Negative Pathogens Including Multi-Drug Resistant Bacteria: Structure Activity Relationship
摘要:The Structure-Activity Relationship (Sar) For A Novel Series Of Catechol Conjugated Siderophore Cephalosporins Is Described With Their In Vitro Activities Against Multi-Drug Resistant Gram-Negative Pathogens Including Pseudomonas Aeruginosa,Acinetobacter Baumannii,Stenotrophomonas Maltophilia And Enterobacteriaceae. Cefiderocol (3) Was One Of The Best Molecules Which Displayed Well-Balanced And Potent Activities Against Multi-Drug Resistant Gram-Negative Pathogens Including Carbapenem Resistant Bacteria Among The Prepared Compounds With The Modified C-7 Side Chain And The Modified C-3 Side Chain. Cefiderocol (3) Is A Highly Promising Parenteral Cephalosporin For The Treatment Of Multi-Drug Resistant Gram-Negative Infection. (C) 2018 Elsevier Masson Sas. All Rights Reserved.
Doi:10.1016/j.Ejmech.2018.06.014

专利信息

专利号:US-2023398101-A1
优先权日:2022-06-09
标题 :Co-agents as Therapy Against Anaerobic Pathogens
发明人：PACE JOHN LEE; HARTSELL THERESA LYNN
权利人:FLEURIR ABX LLC
摘要:Co-agent combinations and/or formulations herein unexpectedly display significantly better antimicrobial activity (e.g., more efficacy and/or more potency) against anaerobic pathogens not previously considered targets. With three or more co-agents, selected from a group of a fosfomycin, a diaminopyridine, a sulfonamide, a beta lactam antibacterial, a bacterial beta-lactamase inhibitor, a bacterial fosfomycin-modifying enzyme, and a bacterial peptidoglycan synthesis inhibitor, the therapeutic potential of the three or more co-agents is expanded by targeting a broader spectrum of pathogens. Co-agents, by unexpected synergistic action in an anaerobic environment, are now active and efficacious against difficult to treat pathogenic anaerobes (including anaerobes that cannot utilize oxygen and/or reside in an anaerobic environment, some being inhibited by oxygen), as well as pathogens considered resistant or intolerant to at least one of the co-agents when used singly in an anaerobic environment. Some co-agent combinations and/or formulations contain one or more existing antibiotic agents being repurposed for utility against difficult to treat anaerobic pathogens.