新制备的 3-氮杂双环[3.2.2]壬烷的抗原生动物效力。
The antiprotozoal potencies of newly prepared 3-azabicyclo[3.2.2]nonanes.
机构信息
Center for Research in Molecular Medicine, The University of Lahore, Lahore, Pakistan.
Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Schubertstrasse 1, 8010, Graz, Austria.
出版信息
Arch Pharm Res. 2016 Oct;39(10):1391-1403. doi: 10.1007/s12272-016-0826-5. Epub 2016 Sep 1.
3-Azabicyclo[3.2.2]nonanes are already reported as antiprotozoal agents. Structural variations were performed by attachment of several basic side chains, being part of drugs in use, to the ring nitrogen. The structures of the new compounds were established using one and two dimensional NMR measurements. All compounds were investigated for their antiplasmodial and antitrypanosomal activities against Plasmodium falciparum K (multiresistant) and Trypanosoma brucei rhodesiense. Their cytotoxicity was assessed against L6 cells. The results are compared to the activities of formerly synthesized compounds. Structure-activity relationships are discussed.
3-氮杂双环[3.2.2]壬烷已被报道具有抗原生动物作用。通过将几种碱性侧链连接到环氮原子上，对其结构进行了改变，这些碱性侧链是现有药物的一部分。利用一维和二维 NMR 测量方法确定了新化合物的结构。所有化合物均针对抗氯喹的恶性疟原虫 K（多药耐药）和罗得西亚锥虫进行了抗疟原虫和抗锥虫活性的检测。用 L6 细胞评估了它们的细胞毒性。将结果与以前合成的化合物的活性进行了比较。讨论了结构-活性关系。
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