当前位置: X-MOL 学术Arch. Pharm. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Evaluation of the antiparasitic activities of imidazol‐2‐ylidene–gold(I) complexes
Archiv der Pharmazie ( IF 5.1 ) Pub Date : 2020-03-09 , DOI: 10.1002/ardp.201900363
Waleed S Koko 1 , Jana Jentzsch 2 , Hussein Kalie 3 , Rainer Schobert 3 , Klaus Ersfeld 2 , Ibrahim S Al Nasr 1, 4 , Tariq A Khan 5 , Bernhard Biersack 3
Affiliation  

A series of cationic gold(I)–carbene complexes with various 4,5‐diarylimidazolylidene ligands were either newly prepared or repurposed for testing against protozoal Leishmania major, Toxoplasma gondii, and Trypanosoma brucei parasites. The syntheses of the new complexes 1b and 1c were described. Ferrocene compound 1a showed the highest activities against L. major amastigotes and T. gondii and distinct selectivity for T. gondii cells when compared with the activity against nonmalignant Vero cells. The ferrocene derivatives 1a–c are generally more active against the L. major amastigotes and the T. gondii tachyzoites than the other tested anisyl gold complexes and the approved drugs atovaquone and amphotericin B. Compounds 1a and 1e showed the highest selectivities for L. major amastigotes. Compounds 1d and 1f showed the highest selectivities for L. major promastigotes; 1f was the most active compound against L. major promastigotes of this series of compounds. The 3,4,5‐trimethoxyphenyl analog 1b also exhibited a much greater selectivity for T. b. brucei cells when compared with its activity against human HeLa cells.

中文翻译:

咪唑-2-亚基-金(I)配合物抗寄生虫活性的评价

一系列具有各种 4,5-二芳基咪唑亚基配体的阳离子金 (I)-卡宾配合物是新制备的或重新用于测试原生动物利什曼原虫、弓形虫和布氏锥虫寄生虫的。描述了新配合物 1b 和 1c 的合成。与对非恶性 Vero 细胞的活性相比,二茂铁化合物 1a 对主要无鞭毛体和弓形虫的活性最高,对弓形虫细胞具有明显的选择性。二茂铁衍生物 1a-c 通常比其他测试的茴香金配合物和批准的药物 atovaquone 和两性霉素 B 对 L. major amastigotes 和 T. gondii tachyzoites 更具活性。 化合物 1a 和 1e 对 L. Major 表现出最高的选择性无鞭毛体。化合物 1d 和 1f 对 L 显示出最高的选择性。主要的前鞭毛体;1f 是该系列化合物中对抗 L.主要前鞭毛体最有效的化合物。3,4,5-三甲氧基苯基类似物 1b 也对 T. b 表现出更大的选择性。与它对人类 HeLa 细胞的活性相比,布鲁氏细胞。
更新日期:2020-03-09
down
wechat
bug