氮杂双环壬烷嘧啶类化合物的合成及抗原生动物活性。
Synthesis and Antiprotozoal Activity of Azabicyclo-Nonane Pyrimidine Hybrids.
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 Dec 30;28(1):307. doi: 10.3390/molecules28010307.
2,4-Diaminopyrimidines and (dialkylamino)azabicyclo-nonanes possess activity against protozoan parasites. A series of fused hybrids were synthesized and tested in vitro against pathogens of malaria tropica and sleeping sickness. The activities and selectivities of compounds strongly depended on the substitution pattern of both ring systems as well as on the position of the nitrogen atom in the bicycles. The most promising hybrids of 3-azabicyclo-nonane with 2-aminopyrimidine showed activity against NF54 in submicromolar concentration and high selectivity. A hybrid with pyrrolidino substitution of the 2-azabicyclo-nonane as well as of the pyrimidine moiety exhibited promising activity against the multiresistant K1 strain of . A couple of hybrids of 2-azabicyclo-nonanes with 2-(dialkylamino)pyrimidines possessed high activity against STIB900 and good selectivity.
2,4-二氨基嘧啶和（二烷基氨基）氮杂双环壬烷具有抗原生动物寄生虫的活性。合成了一系列融合的杂合体，并在体外对热带疟原虫和昏睡病的病原体进行了测试。化合物的活性和选择性强烈依赖于两个环系的取代模式以及自行车中氮原子的位置。具有 3-氮杂双环壬烷和 2-氨基嘧啶的最有前途的杂合体在亚毫摩尔浓度下对 NF54 表现出活性和高选择性。具有吡咯烷取代的 2-氮杂双环壬烷和嘧啶部分的杂合体对多耐药的 K1 株表现出有希望的活性。一些具有 2-（二烷基氨基）嘧啶的 2-氮杂双环壬烷的杂合体对 STIB900 具有高活性和良好的选择性。
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