Synthesis and in vivo antimalarial evaluation of novel hydroxyethylamine derivatives.

Abstract

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.

• Authors: Mariana Conceição de Souza, Triciana Gonçalves-Silva, Marcele Moreth, Claudia R B Gomes, Carlos Roland Kaiser, Maria das Graças Muller de Oliveira Henriques, Marcus V N de Souza
• Journal: Medicinal chemistry (Shariqah (United Arab Emirates)) (Med Chem) Vol. 8 Issue 2 Pg. 266-72 (Mar 2012) ISSN: 1875-6638 [Electronic] Netherlands
• PMID: 22385178 (Publication Type: Evaluation Study, Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antimalarials
• Ethylamines

Topics

• Animals
• Antimalarials (chemical synthesis, chemistry, pharmacology)
• Dose-Response Relationship, Drug
• Ethylamines (chemical synthesis, chemistry, pharmacology)
• Mice
• Molecular Structure
• Parasitemia (drug therapy, metabolism)
• Parasitic Sensitivity Tests
• Plasmodium berghei (drug effects, metabolism)
• Structure-Activity Relationship