Linear and cyclic dipeptides with antimalarial activity.
Several natural and synthetic polypeptides possess important antimalarial activity. Shorter peptides with potent antimalarial activity have also been described, among them linear di-, tri-, tetra- and pentapeptides and their cyclic analogs. In an attempt to find dipeptides with antimalarial activities we show that linear and cyclic dipeptides, the latter known as diketopiperazines, still retain the fundamental core to preserve antimalarial activity. Thirteen linear dipeptides and ten diketopiperazines were investigated. Eight linear dipeptides showed IC(50) values between 2.78 and 7.07 μM, while eight diketopiperazines were also active with IC(50) values between 2.26 and 4.26 μM on Plasmodium berghei schizont cultures.
Centro de Investigaciones Químicas, Universidad Autónoma del Estado de Morelos, Avenida Universidad 1001, Col. Chamilpa, Cuernavaca, Morelos 62209, Mexico.
Lemuel
L
Pérez-Picaso
Horacio F
HF
Olivo
Rocío
R
Argotte-Ramos
María
M
Rodríguez-Gutiérrez
María Yolanda
MY
Rios
D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D018360:Crystallography, X-Ray; D004151:Dipeptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D008968:Molecular Conformation; D010456:Peptides, Cyclic / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D010962:Plasmodium berghei / Q000187:drug effects
D000962:Antimalarials; D004151:Dipeptides; D010456:Peptides, Cyclic