Synthesis of Cyclic Peptides as Potential Anti-Malarials
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Updated: Feb 14, 2026

Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers
Published on: September 19, 2022
Catherine Fagundez1, Diver Sellanes1, Gloria Serra1
1Cátedra de Química Farmacéutica, (DQO), Facultad de Química , Universidad de la República , Gral. Flores 2124 , CP 11800 , Montevideo , Uruguay.
Abstract:
The results from the synthesis of peptides by Fmoc/SPPS on a 2-CTC resin and then lactamization in solution or solid phase for the preparation of cyclopeptides are presented. Both procedures allow the synthesis of the desired compounds in good to very good yield and with high cyclization efficiency for on-resin macrocyclization. In addition, the activities of the corresponding cyclopeptides against the chloroquine-resistant K1 strain of Plasmodium falciparum were evaluated. Cyclo-Cys(Trt)-Gly-Thr( tBu)-Gly-Cys(Trt)-Gly showed potent in vitro and selective activity against this parasite, EC50 = 28 nM.
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