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


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


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.

1  Laboratorio de Química Farmacéutica (DQO), Facultad de Química, Universidad de la República, Gral. Flores 2124, Montevideo, CP 11800, Uruguay

2  Instituto de Física de São Carlos, Universidade de São Paulo, São Paulo, Brazil

3  Faculty of Infectious & Tropical Disease, The London School of Hygiene & Tropical Medicine (LSHTM), Keppel Street, London, WC1E 7HT, U.K.

4  School of Medicine, University of California San Diego, La Jolla, California 92093, United States

5  Diseases of the Developing World (DDW), Tres Cantos Medicines Development Campus, GlaxoSmithKline, Tres Cantos, Spain

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