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

页码：2279 / 2294

页数：16

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