📜1,3-二溴苯置于tris-(Dibenzylideneacetone)Dipalladium(0),1,1'-双(二苯膦基)二茂铁二氯化钯(II)二氯甲烷复合物,Potassium Tert-Butylate,Potassium Acetate,4,5-双二苯基膦-9,9-二甲基氧杂蒽体系中,用 1,4-二氧六环,甲苯 作为反应溶剂,化学反应 6.0H,反应生成 3-码啉苯硼酸四甲基二酯
参考文献:Protozoan Parasite Growth Inhibitors Discovered By Cross-Screening Yield Potent Scaffolds For Lead Discovery
标题:Protozoan Parasite Growth Inhibitors Discovered By Cross-Screening Yield Potent Scaffolds For Lead Discovery
摘要:Tropical Protozoal Infections Are A Significant Cause Of Morbidity And Mortality Worldwide; Four In Particular (Human African Trypanosomiasis (Hat),Chagas Disease,Cutaneous Leishmaniasis,And Malaria) Have An Estimated Combined Burden Of Over 87 Million Disability-Adjusted Life Years. New Drugs Are Needed For Each Of These Diseases,Building On The Previous Identification Of Neu-617 (1) As A Potent And Nontoxic Inhibitor Of Proliferation For The Hat Pathogen (Trypanosoma Brucei),We Have Now Tested This Class Of Analogs Against Other Protozoal Species: T. Cruzi (Chagas Disease),Leishmania Major (Cutaneous Leishmaniasis),And Plasmodium Falciparum (Malaria). Based On Hits Identified In This Screening Campaign,We Describe The Preparation Of Several Replacements For The Quinazoline Scaffold And Report These Inhibitors' Biological Activities Against These Parasites. In Doing This,We Have Identified Several Potent Proliferation Inhibitors For Each Pathogen,Such As 4-(3-Chloro-4-((3-Fluorobenzyl)Oxy)Phenyl)Amino)-6-(4-((4-Methyl-1,4-Diazepan-1-yl)Sulfonyl)Phenyl)Quinoline-3-Carbonitrile (Neu-924,83) For T. Cruzi And N-(3-Chloro-4-((3-Fluorobenzypoxy)Phenyl)-7-(4-((4-Methyl-1,4-Diazepan-1-yl)Sulfonyl)Phenyl)Cinnolin-4-Amine (Neu-1017,68) For L. Major And P. Falciparum.
DOI:10.1021/acs.Jmedchem.5B00515