Bartlett M S, Edlind T D, Durkin M M, Shaw M M, Queener S F, Smith J W
Indiana University School of Medicine, Indianapolis 46202-5250.
Antimicrob Agents Chemother. 1992 Apr;36(4):779-82. doi: 10.1128/AAC.36.4.779.
Nine antimicrotubule benzimidazole derivatives tested in a Pneumocystis carinii culture system with human embryonic lung fibroblast monolayers inhibited organism proliferation. The concentrations of drugs inhibitory in culture ranged from 10 to 0.1 micrograms/ml, with thiabendazole being the least effective (10 micrograms/ml) and parbendazole being the most effective (0.1 microgram/ml). The parent compound, benzimidazole, was inactive at 10 micrograms/ml. Demonstration that this group of compounds has activity against P. carinii provides a new potential target that can be exploited, the microtubules. Also, the variability in the effectiveness of the compounds provides the basis for studies of structure-activity relationships, which were initiated in this study.
在卡氏肺孢子虫培养系统中，用人胚肺成纤维细胞单层对9种抗微管苯并咪唑衍生物进行测试，结果显示这些衍生物可抑制虫体增殖。培养中具有抑制作用的药物浓度范围为10至0.1微克/毫升，其中噻苯达唑效果最差（10微克/毫升），而帕苯达唑效果最佳（0.1微克/毫升）。母体化合物苯并咪唑在10微克/毫升时无活性。这组化合物对卡氏肺孢子虫具有活性，这表明微管可作为一个新的潜在靶点进行开发。此外，这些化合物有效性的差异为结构-活性关系研究提供了基础，本研究已启动相关研究。
