Antischistosomal agents: state of art and perspectives

被引:69
|
作者
Lago, Eloi M. [1 ]
Xavier, Rogerio P. [1 ]
Teixeira, Thaina R. [1 ]
Silva, Livia M. [2 ]
da Silva Filho, Ademar A. [2 ]
de Moraes, Josue [1 ]
机构
[1] Univ Universus Veritas UNIVERITAS UNG, Nucl Pesquisa Doencas Negligenciadas, Praca Tereza Cristina 229, BR-07023070 Guarulhos, SP, Brazil
[2] Univ Fed Juiz de Fora, Dept Ciencias Farmaceut, Juiz De Fora, MG, Brazil
基金
巴西圣保罗研究基金会;
关键词
chemogenomics; drug discovery; drug repositioning; druggability; high-throughput screening; Hit; lead; molecular modeling; ADULT SCHISTOSOMA-MANSONI; IN-VIVO ACTIVITIES; ANTIINFLAMMATORY DRUG DICLOFENAC; SURFACE-MEMBRANE DAMAGE; ARACHIDONIC-ACID; CYCLOSPORINE-A; ULTRASTRUCTURAL ANALYSIS; ANTIMICROBIAL PEPTIDE; ANTHELMINTIC ACTIVITY; EGG-PRODUCTION;
D O I
10.4155/fmc-2017-0112
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Praziquantel has remained the drug of choice for schistosomiasis chemotherapy for almost 40 years. The pressing need to develop a new antischistosomal drug may necessitate exploring and filtering chemotherapeutic history to search for the most promising ones. In this context, this review attempts to summarize all progress made in schistosomiasis chemotherapy from the early 20th century (mid-1910s) to 2016. We gathered almost 100 compounds providing information on therapeutic action, specifically covering at least first in vivo studies in animal model and in vitro. Pharmacokinetic and toxicity profiles of antischistosomal agents were also described. Preclinical studies indicate a handful of promising future candidates.
引用
收藏
页码:89 / 120
页数:32
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