评价新型噻唑烷/噻二唑烷衍生物对隐孢子虫体外发育的疗效，发现与硝基基团无关。
Evaluation of new thiazolide/thiadiazolide derivatives reveals nitro group-independent efficacy against in vitro development of Cryptosporidium parvum.
机构信息
Parasitology Department, Rouen University Hospital and UPRES-EA 4311-IFRMP 23, University of Rouen, Rouen, France.
出版信息
Antimicrob Agents Chemother. 2010 Mar;54(3):1315-8. doi: 10.1128/AAC.00614-09. Epub 2010 Jan 4.
Abstract
Thirty-nine new thiazolide/thiadiazolide compounds were compared with the nitrothiazole nitazoxanide for activity against Cryptosporidium parvum development in HCT-8 cells. Twenty-seven agents exerted > or =90% inhibition. Agents with a lower 50% inhibitory concentration (IC(50)) than nitazoxanide were either NO(2) or halogen 5 substituted on the thiazole moiety. Other 5 substitutions such as methyl, C(3)H(7), C(6)H(11), H, SO(2)CH(3), and SCH(3) negatively impacted activity. Five-substituted deacetylated analogues exhibited higher IC(50)s than their acetylated counterparts. Halogeno-thiazolide/thiadiazolides may provide valuable nitro-free alternatives to nitazoxanide.
摘要
39 种新型噻唑烷/噻二唑烷化合物与硝基噻唑硝唑替硝唑进行了比较，以评估它们对 HCT-8 细胞中隐孢子虫发育的抑制活性。27 种药物的抑制率超过 90%。与硝唑替硝唑相比，50%抑制浓度（IC50）较低的药物要么是噻唑部分的 NO2 或卤素 5 取代，要么是卤素 5 取代。其他 5 取代基，如甲基、C3H7、C6H11、H、SO2CH3 和 SCH3，对活性有负面影响。5 取代的脱乙酰化类似物的 IC50 高于其乙酰化类似物。卤代噻唑烷/噻二唑烷可能为硝唑替硝唑提供有价值的无硝基替代品。
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