Affiliation:
1. Centre of Excellence for Pharmaceutical Sciences North-West University Potchefstroom 2520 South Africa
2. Center for Discovery and Innovation in Parasitic Diseases University of California San Diego 9500 Gilman Drive La Jolla CA 92093 USA
Abstract
AbstractNagana and Human African Trypanosomiasis (HAT), caused by (sub)species of Trypanosoma, are diseases that impede human and animal health, and economic growth in Africa. The few drugs available have drawbacks including suboptimal efficacy, adverse effects, drug resistance, and difficult routes of administration. New drugs are needed. A series of 20 novel quinolone compounds with affordable synthetic routes was made and evaluated in vitro against Trypanosoma brucei and HEK293 cells. Of the 20 compounds, 12 had sub‐micromolar potencies against the parasite (EC50 values=0.051–0.57 μM), and most were non‐toxic to HEK293 cells (CC50 values>5 μM). Two of the most potent compounds presented sub‐micromolar activities against other trypanosome (sub)species (T. cruzi and T. b. rhodesiense). Although aqueous solubility is poor, both compounds possess good logD values (2–3), and either robust or poor microsomal stability profiles. These varying attributes will be addressed in future reports.
Cited by
1 articles.
订阅此论文施引文献
订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献