合成及对映体杀配子体药物（oryzalin）抗弓形虫的评价。
Synthesis and evaluation of oryzalin analogs against Toxoplasma gondii.
机构信息
Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210-1291, USA.
出版信息
Bioorg Med Chem Lett. 2010 Sep 1;20(17):5179-83. doi: 10.1016/j.bmcl.2010.07.003. Epub 2010 Jul 8.
The synthesis and evaluation of 20 dinitroanilines and related compounds against the obligate intracellular parasite Toxoplasma gondii is reported. Using in vitro cultures of parasites in human fibroblasts, we determined that most of these compounds selectively disrupted Toxoplasma microtubules, and several displayed sub-micromolar potency against the parasite. The most potent compound was N(1),N(1)-dipropyl-2,6-dinitro-4-(trifluoromethyl)-1,3-benzenediamine (18b), which displayed an IC(50) value of 36 nM against intracellular T. gondii. Based on these data and another recent report [Ma, C.; Tran, J.; Gu, F.; Ochoa, R.; Li, C.; Sept, D.; Werbovetz, K.; Morrissette, N. Antimicrob. Agents Chemother. 2010, 54, 1453], an antimitotic structure-activity relationship for dinitroanilines versus Toxoplasma is presented.
报道了 20 种邻二硝基苯胺及其相关化合物的合成和评估，以对抗专性细胞内寄生虫刚地弓形虫。我们通过人成纤维细胞中的寄生虫体外培养，确定这些化合物大多数都能选择性地破坏刚地弓形虫微管，其中一些对寄生虫显示出亚微摩尔的效力。最有效的化合物是 N(1)，N(1)-二丙基-2,6-二硝基-4-(三氟甲基)-1,3-苯二胺（18b），对细胞内刚地弓形虫的 IC(50)值为 36 nM。基于这些数据和另一个最近的报告[Ma, C.; Tran, J.; Gu, F.; Ochoa, R.; Li, C.; Sept, D.; Werbovetz, K.; Morrissette, N. Antimicrob. Agents Chemother. 2010, 54, 1453]，提出了邻二硝基苯胺对抗刚地弓形虫的抗有丝分裂构效关系。
Zotero 插件