Decsi Balázs, Krammer Réka, Hegedűs Kristóf, Ender Ferenc, Gyarmati Benjámin, Szilágyi András, Tőtős Róbert, Katona Gabriel, Paizs Csaba, Balogh György T, Poppe László, Balogh-Weiser Diána
Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, Műegyetem rkp. 3, 1111 Budapest, Hungary.
SpinSplit Llc., Leonardo da Vinci u. 43b, 1082 Budapest, Hungary.
Micromachines (Basel). 2019 Oct 1;10(10):668. doi: 10.3390/mi10100668.
Biomimetic oxidation of drugs catalyzed by metalloporphyrins can be a novel and promising way for the effective and sustainable synthesis of drug metabolites. The immobilization of 5,10,15,20-tetrakis(2,3,4,5,6-pentafluorophenyl)iron(II) porphyrin (FeTPFP) and 5,10,15,20-tetrakis-(4-sulfonatophenyl)iron(II) porphyrin (FeTSPP) via stable covalent or rapid ionic binding on aminopropyl-functionalized magnetic nanoparticles (MNPs-NH) were developed. These immobilized catalysts could be efficiently applied for the synthesis of new pharmaceutically active derivatives and liver related phase I oxidative major metabolite of an antiarrhythmic drug, amiodarone integrated in a continuous-flow magnetic chip reactor (Magnechip).
金属卟啉催化的药物仿生氧化可能是一种有效且可持续地合成药物代谢物的新颖且有前景的方法。通过稳定的共价键或快速离子键合将5,10,15,20-四（2,3,4,5,6-五氟苯基）铁（II）卟啉（FeTPFP）和5,10,15,20-四（4-磺基苯基）铁（II）卟啉（FeTSPP）固定在氨丙基功能化磁性纳米颗粒（MNPs-NH）上。这些固定化催化剂可有效地用于合成新的药物活性衍生物以及抗心律失常药物胺碘酮的肝脏相关I相氧化主要代谢物，该过程集成在连续流磁性芯片反应器（Magnechip）中。
