Department of Chemistry, Adelphi University, 1 South Avenue, Garden City, NY 11530, United States.
Department of Chemistry, Adelphi University, 1 South Avenue, Garden City, NY 11530, United States.
Bioorg Med Chem Lett. 2014 Feb 15;24(4):1080-4. doi: 10.1016/j.bmcl.2014.01.014. Epub 2014 Jan 13.
Trichomonas vaginalis continues to be a major health problem with drug-resistant strains increasing in prevalence. Novel antitrichomonal agents that are mechanistically distinct from current therapies are needed. The NIH Clinical Compound Collection was screened to find inhibitors of the uridine ribohydrolase enzyme required by the parasite to scavenge uracil for its growth. The proton-pump inhibitors omeprazole, pantoprazole, and rabeprazole were identified as inhibitors of this enzyme, with IC50 values ranging from 0.3 to 14.5 μM. This suggests a molecular mechanism for the in vitro antitrichomonal activity of these proton-pump inhibitors, and may provide important insights toward structure-based drug design.
阴道毛滴虫仍然是一个主要的健康问题，具有耐药性的菌株越来越普遍。需要新型的、与现有治疗方法在机制上不同的抗滴虫药物。美国国立卫生研究院临床化合物库被筛选，以寻找寄生虫生长所需的尿苷核糖水解酶的抑制剂。质子泵抑制剂奥美拉唑、泮托拉唑和雷贝拉唑被鉴定为该酶的抑制剂，IC50 值范围为 0.3 至 14.5 μM。这表明这些质子泵抑制剂在体外抗滴虫活性的分子机制，并可能为基于结构的药物设计提供重要的见解。
