title: 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.affiliation: Instituto de Tecnologia em Fármacos-Farmanguinhos, FioCruz-Fundacao Oswaldo Cruz, R. Sizenando Nabuco, 100, Manguinhos, 21041-250, Rio de Janeiro, RJ, Brazil.
authors.forename: Mariana Conceição
authors.initials: MC
authors.lastname: de Souza
authors.forename: Triciana
authors.initials: T
authors.lastname: Gonçalves-Silva
authors.forename: Marcele
authors.initials: M
authors.lastname: Moreth
authors.forename: Claudia R B
authors.initials: CR
authors.lastname: Gomes
authors.forename: Carlos Roland
authors.initials: CR
authors.lastname: Kaiser
authors.forename: Maria das Graças Muller
authors.initials: Md
authors.lastname: de Oliveira Henriques
authors.forename: Marcus V N
authors.initials: MV
authors.lastname: de Souza
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D005021:Ethylamines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D015394:Molecular Structure; D018512:Parasitemia / Q000188:drug therapy* / Q000378:metabolism; D021261:Parasitic Sensitivity Tests; D010962:Plasmodium berghei / Q000187:drug effects* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D005021:Ethylamines