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J Med Chem. 2013 Oct 24;56(20):7715-8. doi: 10.1021/jm400443k. Epub 2013 Aug 27.
Drug development for neglected tropical diseases, defined as a collection of infectious diseases affecting over 4 billion people worldwide (especially endemic to poverty-stricken populations in underdeveloped regions of Africa, Asia, the Pacific Rim, and Latin America), has been underfunded and stagnant. A much needed resurgence of R&D activity in this area is currently developing. Target-directed screening and whole-cell phenotypic screening represent two complementary approaches to discover viable new starting point scaffolds for medicinal chemistry optimization. This editorial will provide introductory comments to a series of six miniperspectives that focus on the special challenges faced by scientists in discovering potential new chemical leads that could be optimized into promising clinical candidates for neglected tropical diseases.
用于治疗被忽视热带病的药物研发一直处于资金不足和停滞的状态,这些疾病是指一组影响全球超过 40 亿人的传染病(尤其流行于非洲、亚洲、环太平洋地区和拉丁美洲的贫困地区)。目前,该领域急需重振研发活动。针对目标的筛选和全细胞表型筛选代表了两种互补的方法,可以发现可行的新起点支架,用于药物化学优化。本社论将对六篇小综述系列提供介绍性评论,这些综述主要关注科学家在发现可能的新化学先导物方面所面临的特殊挑战,这些先导物可以被优化成有前途的治疗被忽视热带病的临床候选药物。