Synthesis, Profiling, and in Vivo Evaluation of Cyclopeptides Containing N-Methyl Amino Acids as Antiplasmodial Agents

被引：12

作者：

Fagundez, Catherine ^{[1
]}

Sellanes, Diver ^{[1
]}

Pena, Stella ^{[1
]}

Scarone, Laura ^{[1
]}

Aguiar, Anna C. C. ^{[2
]}

de Souza, Juliana O. ^{[2
]}

Guido, Rafael V. C. ^{[2
]}

Stewart, Lindsay ^{[3
]}

Yardley, Vanessa ^{[3
]}

Ottilie, Sabine ^{[4
]}

Winzeler, Elizabeth A. ^{[4
]}

Gamo, Francisco-J. ^{[5
]}

Sanz, Laura M. ^{[5
]}

Serra, Gloria L. ^{[1
]}

机构：

[1] Univ Republica, Fac Quim, Lab Quim Farmaceut DQO, Gral Flores 2124, Montevideo 11800, Uruguay

[2] Univ Sao Paulo, Inst Fis Sao Carlos, Sao Paulo, Brazil

[3] LSHTM, Fac Infect & Trop Dis, Keppel St, London WC1E 7HT, England

[4] Univ Calif San Diego, Sch Med, La Jolla, CA 92093 USA

[5] GlaxoSmithKline, DDW, Tres Cantos Medicines Dev Campus, Tres Cantos, Spain

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2019年 / 10卷 / 01期

基金：

巴西圣保罗研究基金会;

关键词：

Antiplasmodial; cyclopeptides; synthesis; physicochemical properties; CYCLIC-PEPTIDES; ARTEMISININ; RESISTANCE; MACROCYCLES; DISCOVERY; MALARIA;

D O I：

10.1021/acsmedchemlett.8b00543

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Malaria is a major tropical disease where important needs are to mitigate symptoms and to prevent the establishment of infection. Cyclopeptides containing N-methyl amino acids with in vitro activity against erythrocytic forms as well as liver stage are presented. The synthesis, parasitological characterization, physicochemical properties, in vivo evaluation, and mice pharmacokinetics are described.

引用

页码：137 / 141

页数：9

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