Bell C A, Cory M, Fairley T A, Hall J E, Tidwell R R
Department of Parasitology and Laboratory Practice, School of Public Health, University of North Carolina, Chapel Hill 27599.
Antimicrob Agents Chemother. 1991 Jun;35(6):1099-107. doi: 10.1128/AAC.35.6.1099.
1,5-Di(4-amidinophenoxy)pentane (pentamidine) and 38 analogs of pentamidine were screened for in vitro activity against the enteric protozoan Giardia lamblia WB (ATCC 30957). All compounds were active against G. lamblia as measured by a [methyl-3H]thymidine incorporation assay. Antigiardial activity varied widely, with 50% inhibitory concentrations (IC50s) ranging from 0.51 +/- 0.13 microM (mean +/- standard deviation) for the most active compound to over 100.0 microM for the least active compounds. The IC50 of the most potent antigiardial agent, 1,3-di(4-amidino-2-methoxyphenoxy)propane compared favorably with the IC50s of the compounds currently used to treat giardiasis, i.e., furazolidone (1.0 +/- 0.03 microM), metronidazole (2.1 +/- 0.80 microM), quinacrine HCl (0.03 +/- 0.02 microM), and tinidazole (0.78 +/- 0.48 microM). A mode of antigiardial activity for these compounds was suggested by the correlation observed between antigiardial activity and the binding of the compounds to calf thymus DNA and poly(dA).poly(dT).
对1,5 - 二（4 - 脒基苯氧基）戊烷（喷他脒）及其38种类似物进行了体外抗肠道原生动物蓝氏贾第鞭毛虫WB（ATCC 30957）活性的筛选。通过[甲基 - 3H]胸苷掺入试验测定，所有化合物均对蓝氏贾第鞭毛虫有活性。抗贾第虫活性差异很大，50%抑制浓度（IC50）范围从活性最强的化合物的0.51±0.13微摩尔（平均值±标准差）到活性最弱的化合物的超过100.0微摩尔。最有效的抗贾第虫药物1,3 - 二（4 - 脒基 - 2 - 甲氧基苯氧基）丙烷的IC50与目前用于治疗贾第虫病的化合物的IC50相比具有优势，即呋喃唑酮（1.0±0.03微摩尔）、甲硝唑（2.1±0.80微摩尔）、盐酸阿的平（0.03±0.02微摩尔）和替硝唑（0.78±0.48微摩尔）。这些化合物的抗贾第虫活性模式是由抗贾第虫活性与化合物与小牛胸腺DNA和聚（dA）·聚（dT）的结合之间观察到的相关性所提示的。
