Synthesis and in vivo antimalarial evaluation of novel hydroxyethylamine derivatives

• Published in: Medicinal chemistry (Shp-sariqah, United Arab Emirates) Vol. 8; no. 2; p. 266
• Main Authors: de Souza, Mariana Conceição, Gonçalves-Silva, Triciana, Moreth, Marcele, Gomes, Claudia R B, Kaiser, Carlos Roland, de Oliveira Henriques, Maria das Graças Muller, de Souza, Marcus V N
• Format: Journal Article
• Language: English
• Published: Netherlands 01.03.2012
• Subjects: Animals; Antimalarials - chemical synthesis; Antimalarials - chemistry; Antimalarials - pharmacology; Dose-Response Relationship, Drug; Ethylamines - chemical synthesis; Ethylamines - chemistry; Ethylamines - pharmacology; Mice; Molecular Structure; Parasitemia - drug therapy; Parasitemia - metabolism; Parasitic Sensitivity Tests; Plasmodium berghei - drug effects; Plasmodium berghei - metabolism; Structure-Activity Relationship
• ISSN: 1875-6638
• DOI: 10.2174/157340612800493638

A series of hydroxyethylamines has been synthesized from the reaction of (2S,3S )Boc-phenylalanine epoxide with alkyl amines in good yields and evaluated for their in vivo antimalarial activity in mice. Compound 4g presented better activity then the reference artesunate in percentage of inhibition of parasitemia in treated P. berghei-infected mice and compare to the activity of artesunate in the survival of mice 14 days after infection. In addiction, no hemolytic activity was found, which supports that inhibition of parasitemia is due to antimalarial activity. The compound 4g inhibited the differentiation to schizonts suggesting that parasite metabolism is a possible target of 4g. These results indicate that this class of compound possesses promising perspectives for the development of new antimalarial drugs.