📜Tert-Butyl 4-(2-Nitropyridin-4-yl)Piperazine-1-Carboxylate置于palladium On Activated Charcoal,氢气,溶剂黄146体系中,用 甲醇 作为反应溶剂,化学反应 4.0H,反应生成 1-Boc-4-(2-氨基-4-吡啶基)哌嗪
参考文献:Antimalarial Lead-Optimization Studies On A 2,6-Imidazopyridine Series Within A Constrained Chemical Space To Circumvent Atypical Dose-response Curves Against Multidrug Resistant Parasite Strains
标题:Antimalarial Lead-Optimization Studies On A 2,6-Imidazopyridine Series Within A Constrained Chemical Space To Circumvent Atypical Dose-response Curves Against Multidrug Resistant Parasite Strains
摘要:A Lead-Optimization Program Around A 2,6-Imidazopyridine Scaffold Was Initiated Based On The Two Early Lead Compounds,1 And 2,That Were Shown To Be Efficacious In An In Vivo Humanized Plasmodium Falciparum Nodscidil2R Gamma Null Mouse Malaria Infection Model. The Observation Of Atypical Dose-Response Curves When Some Compounds Were Tested Against Multidrug Resistant Malaria Parasite Strains Guided The Optimization Process To Define A Chemical Space That Led To Typical Sigmoidal Dose-Response And Complete Kill Of Multidrug Resistant Parasites. After A Structure And Property Analysis Identified Such A Chemical Space,Compounds Were Prepared That Displayed Suitable Activity,Adme,And Safety Profiles With Respect To Cytotoxicity And Herg Inhibition.
DOI:10.1021/acs.Jmedchem.8B01333