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

Catherine Fagundez ; Diver Sellanes ; Stella Peña ; Laura Scarone ; Anna CC Aguiar ; Juliana O de Souza ; Rafael VC Guido ; Lindsay Stewart ; Vanessa Yardley ORCID logo ; Sabine Ottilie ; +4 more... Elizabeth A Winzeler ; Francisco-J Gamo ; Laura M Sanz ; Gloria L Serra ; (2019) Synthesis, Profiling, and in Vivo Evaluation of Cyclopeptides Containing N-Methyl Amino Acids as Antiplasmodial Agents. ACS medicinal chemistry letters, 10 (1). pp. 137-141. ISSN 1948-5875 DOI: 10.1021/acsmedchemlett.8b00543
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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.


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