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

Author(s):Show less -

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]

Affiliation

^[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

• Document type: Journal article
• Source: ACS Medicinal Chemistry Letters; v. 10, n. 1, p. 137-141, JAN 2019.
• Web of Science Citations: 1

Abstract

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)

• FAPESP's process: 13/07600-3 - CIBFar - Center for Innovation in Biodiversity and Drug Discovery
• Grantee: Glaucius Oliva
• Support Opportunities: Research Grants - Research, Innovation and Dissemination Centers - RIDC