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

Autor(es):Mostrar menos -

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]

Afiliação do(s) autor(es)

^[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

• Tipo de documento: Artigo Científico
• Fonte: ACS Medicinal Chemistry Letters; v. 10, n. 1, p. 137-141, JAN 2019.
• Citações Web of Science: 1

Resumo

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. (AU)

• Processo FAPESP: 13/07600-3 - CIBFar - Centro de Inovação em Biodiversidade e Fármacos
• Beneficiário: Glaucius Oliva
• Modalidade de apoio: Auxílio à Pesquisa - Centros de Pesquisa, Inovação e Difusão - CEPIDs