Structure-activity relationship of 4-azaindole-2-piperidine derivatives as agents against Trypanosoma cruzi

被引：6

作者：

Koovits, Paul J. ^{[1
]}

Dessoy, Marco A. ^{[1
]}

Matheeussen, An ^{[2
]}

Maes, Louis ^{[2
]}

Caljon, Guy ^{[2
]}

Mowbray, Charles E. ^{[3
]}

Kratz, Jadel M. ^{[3
]}

Dias, Luiz C. ^{[1
]}

机构：

[1] Univ Estadual Campinas, UNICAMP, Inst Chem, Rua Josue Castro S-N,Cidade Univ, BR-13083861 Campinas, SP, Brazil

[2] LMPH, Univ Pl 1, B-2610 Antwerp, Belgium

[3] DNDi, 15 Chemin Louis Dunant, CH-1202 Geneva, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2020年 / 30卷 / 01期

基金：

巴西圣保罗研究基金会;

关键词：

Neglected diseases; Chagas disease; Drug discovery; Azaindole; CHAGAS-DISEASE; RANDOMIZED-TRIAL; TRANSMISSION; BENZNIDAZOLE;

D O I：

10.1016/j.bmcl.2019.126779

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The structure-activity relationship of a 4-Azaindole-2-piperidine compound selected from GlaxoSmithKline's recently disclosed open-resource "Chagas box" and possessing moderate activity against Trypanosoma cruzi, the parasite responsible for Chagas disease, is presented. Despite considerable medicinal chemistry efforts, a suitably potent and metabolically stable compound could not be identified to advance the series into in vivo studies. This research should be of interest to those in the area of neglected diseases and in particular anti-kinetoplastid drug discovery.

引用

页数：7

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