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1.
Eur J Med Chem ; 125: 327-334, 2017 Jan 05.
Artigo em Inglês | MEDLINE | ID: mdl-27688187

RESUMO

In this work, the synthesis of a series of 2-arylazoimidazole derivatives 6-20 has been achieved through the reaction of imidazole with aryldiazonium salts, followed by ultrasound-assisted alkylation. This approach has important advantages including higher yield, shorter reaction times and milder reaction conditions. The structures of the compounds obtained were determined by MS, IR; and 1H and 13C NMR. The anti-Trypanosoma cruzi activity of the 15 compounds obtained was evaluated. Two compounds with piperidino substituents in the carboxamide moiety proved to be effective inhibitors of epimastigote proliferation, obtaining inhibition values comparable to those achieved with the reference drug Benznidazole. Besides, these compounds displayed low cytotoxicity on mammalian cells. In vivo, both compounds protected mice against a challenge with a lethal Trypanosoma cruzi strain. These results allow us to propose 2-arylazoimidazoles as lead compounds for the design of novel drugs to treat Chagas' disease.


Assuntos
Doença de Chagas/tratamento farmacológico , Imidazóis/química , Imidazóis/uso terapêutico , Tripanossomicidas/química , Tripanossomicidas/uso terapêutico , Trypanosoma cruzi/efeitos dos fármacos , Alquilação , Animais , Linhagem Celular , Doença de Chagas/parasitologia , Humanos , Imidazóis/farmacologia , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Sonicação , Tripanossomicidas/farmacologia , Trypanosoma cruzi/citologia
2.
Int J Infect Dis ; 61: 51-55, 2017 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-28602764

RESUMO

OBJECTIVE: The occurrence of hantavirus in Sub-Saharan Africa is poorly studied and its clinical implications are unknown. This study aimed to determine the occurrence of hantavirus infection among febrile patients attending an outpatient clinic at a primary health care center located in a suburban area of the city of Maputo in Mozambique. METHODS: Paired acute and convalescent samples from a total of 200 febrile patients aged >5years who were recruited between February 2012 and October 2014 were screened for IgM and IgG antibodies against hantavirus using an ELISA. Acute samples were also screened for malaria and to determine hematological and clinical chemistry parameters. RESULTS: Of the 200 patients enrolled, four had IgM antibodies in their acute sample and IgG antibodies in their convalescent sample, yielding a prevalence rate of 2%. Contact with rodents was higher among IgM-positive participants than IgM-negative participants (50.0% (2/4) vs. 15.3% (30/196)). IgM-positive patients presented significantly higher levels of creatinine and alanine aminotransferase and lower platelet counts than IgM-negative patients. CONCLUSIONS: The findings of this study demonstrate human exposure to hantavirus in Mozambique for the first time; however, further studies should be conducted to investigate its clinical implications.


Assuntos
Anticorpos Antivirais/sangue , Infecções por Hantavirus/epidemiologia , Orthohantavírus , Adulto , Alanina Transaminase/sangue , Ensaio de Imunoadsorção Enzimática , Feminino , Febre/epidemiologia , Febre/virologia , Humanos , Masculino , Pessoa de Meia-Idade , Moçambique/epidemiologia , Prevalência , Adulto Jovem
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