Hits, leads and drugs against malaria through diversity-oriented synthesis

被引：0
|
作者：
Dandapani, Sivaraman [1 ]
Comer, Eamon [1 ]
Duvall, Jeremy R. [1 ]
Munoz, Benito [1 ]
机构：
[1] Broad Inst, Cambridge, MA 02142 USA
来源：
FUTURE MEDICINAL CHEMISTRY | 2012年 / 4卷 / 18期
关键词：
BUILD/COUPLE/PAIR STRATEGY; DISCOVERY; SPIROINDOLONES; ANTIMALARIALS; SCAFFOLDS; LIBRARIES; POTENT; SPACE;
D O I：
10.4155/FMC.12.178
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Malaria is a devastating infectious disease and approximately half the world's population is at risk. Since vaccination is not yet available, small-molecule-based medicines are currently the best option for the treatment of patients suffering from malaria and combating the spread of infection. Development of resistance against existing drugs has created a need for new types of small molecules to be screened against Plasmodium falciparum, the etiological agent of malaria. The advent of diversity-oriented synthesis has enabled access to novel chemical structures. Evaluation of diversity-oriented synthesis compounds in phenotypic assays for growth inhibition of P. falciparum has resulted in novel hits, leads and even investigational drugs against malaria.
引用
收藏
页码：2279 / 2294
页数：16
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