含氮杂环壬烷连接四唑或磺胺核心的抗原生动物活性。
Antiprotozoal Activity of Azabicyclo-Nonanes Linked to Tetrazole or Sulfonamide Cores.
机构信息
Pharmaceutical Chemistry, Institute of Pharmaceutical Sciences, University of Graz, Schubertstraße 1, A-8010 Graz, Austria.
Institute for Chemistry and Technology of Materials (ICTM), Graz University of Technology, Stremayrgasse 9, A-8010 Graz, Austria.
出版信息
Molecules. 2022 Sep 21;27(19):6217. doi: 10.3390/molecules27196217.
-(Aminoalkyl)azabicyclo[3.2.2]nonanes possess antiplasmodial and antitrypanosomal activity. A series with terminal tetrazole or sulfonamido partial structure was prepared. The structures of all new compounds were confirmed by NMR and IR spectroscopy and by mass spectral data. A single crystal structure analysis enabled the distinction between isomers. The antiprotozoal activities were examined in vitro against strains of and (STIB 900). The most active sulfonamide and tetrazole derivates showed activities in the submicromolar range.
（氨烷基）氮杂双环[3.2.2]壬烷具有抗疟原虫和抗锥虫活性。合成了一系列带有末端四唑或磺酰胺部分结构的化合物。所有新化合物的结构均通过 NMR 和 IR 光谱以及质谱数据得到证实。单晶结构分析可区分异构体。对体外培养的 和 （STIB 900）菌株进行了抗原生动物活性检测。最活跃的磺酰胺和四唑衍生物在亚微摩尔范围内表现出活性。
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