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

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.

SUBMITTER: Fagundez C

PROVIDER: S-EPMC6331169 | biostudies-literature | 2019 Jan

REPOSITORIES: biostudies-literature

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

Fagundez Catherine C Sellanes Diver D Peña Stella S Scarone Laura L Aguiar Anna C C ACC de Souza Juliana O JO Guido Rafael V C RVC Stewart Lindsay L Yardley Vanessa V Ottilie Sabine S Winzeler Elizabeth A EA Gamo Francisco-J FJ Sanz Laura M LM Serra Gloria L GL

ACS medicinal chemistry letters 20181226 1

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. ...[more]

PMID: 30655961

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