哌嗪 N-取代萘啶、吡啶并噻吩并嘧啶和吡啶并噻吩并三嗪：对真鲷类肠袋虫有活性的新型抗原虫药
Piperazine N-substituted naphthyridines, pyridothienopyrimidines and pyridothienotriazines: new antiprotozoals active against Philasterides dicentrarchi.
作者信息
Quintela José M, Peinador Carlos, González Liliana, Iglesias Raúl, Paramá Anabel, Alvarez Francisca, Sanmartín Manuel L, Riguera Ricardo
机构信息
Departamento de Qui;mica Fundamental e Industrial, Facultad de Ciencias, Universidad de La Coruña, 15071, La Coruña, Spain.
出版信息
Eur J Med Chem. 2003 Mar;38(3):265-75. doi: 10.1016/s0223-5234(03)00032-1.
New antiprotozoals active against Philasterides dicentrarchi, the causative agent of scuticociliatosis in farmed turbot and Black Sea bass-bream, have been synthesised and tested. The most active compounds posses a piperazine ring, generally N-bonded to the heterocycle, and are the 1,8-naphthyridines, 2f and 5o, the pyridothienopyrimidine (7), and the pyridothienotriazines, 8, 9, 12d, 12f, 12h, 12m and 12k. Pyridothienotriazine (12k) presents the same activity (Lethal Dose, LD=0.8/1.5 mg L(-1)) as the well-known antiparasitics niclosamide and oxyclozanide.
已合成并测试了对养殖大菱鲆和黑海鲈鲷盾纤毛虫病病原体双盘藻（Philasterides dicentrarchi）具有活性的新型抗原生动物药物。最具活性的化合物含有一个哌嗪环，通常与杂环氮键合，包括1,8-萘啶（2f和5o）、吡啶并噻吩并嘧啶（7）以及吡啶并噻吩三嗪（8、9、12d、12f、12h、12m和12k）。吡啶并噻吩三嗪（12k）与著名的抗寄生虫药物氯硝柳胺和奥昔氯生具有相同的活性（致死剂量，LD = 0.8/1.5 mg L(-1)）。
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