Eskitis Institute for Cell and Molecular Therapies, Nathan Campus, Griffith University, Brisbane, QLD, 4111, Australia.
Mini Rev Med Chem. 2013 Apr 1;13(5):730-43. doi: 10.2174/1389557511313050010.
The development of leishmanicidal quinolines and their in vitro (promastigote and amastigote) and, where applicable, in vivo activities are reviewed. This survey provides a direct comparison of bioactivity across different species(e.g. L. donovani, L. amazonensis, L. chagasi, L infantum), and in different animal models (e.g. L. donovani Balb/c mice and L. donovani infected hamsters). The progress of selected quinolines through pre-clinical development and phase I/II trials, and the lead quinoline drugs sitamaquinine and Imiquimod, are discussed in conjunction with delivery systems and combination therapies.
本文综述了杀利什曼原虫喹啉类化合物的发展及其体外(前鞭毛体和无鞭毛体)和(适用时)体内活性。本综述提供了不同种属(例如,利什曼原虫、亚马逊利什曼原虫、恰加斯利什曼原虫、婴儿利什曼原虫)和不同动物模型(例如,感染巴尔通体的利什曼原虫 Balb/c 小鼠和感染巴尔通体的仓鼠)间生物活性的直接比较。本文还讨论了选定喹啉类化合物通过临床前开发和 I/II 期试验的进展,以及先导喹啉药物西米喹酮和咪喹莫特,同时还讨论了传递系统和联合疗法。