Alkyl and dialkylaminoethyl derivatives of 5-amino-2-azabicyclo[3.2.2]nonanes and their antiplasmodial and antitrypanosomal activities.
Eur J Med Chem
; 45(1): 179-85, 2010 Jan.
Article
em En
| MEDLINE
| ID: mdl-19879671
ABSTRACT
N-Alkyl and N-(2-dialkylaminoethyl) derivatives of 5-amino-2-azabicyclo-nonanes were prepared and tested in vitro for their activities against the multidrug-resistant K1 strain of Plasmodium falciparum and Trypanosoma brucei rhodesiense (STIB 900). Most of the new compounds showed lower antitrypanosomal activity than their parent compounds. With respect to their activity against P. falciparum the N-alkyl derivatives exhibited worse selectivity due to decreased antiplasmodial activity or higher cytotoxicity. In comparison all of the new N-(2-dialkylaminoethyl) analogues possessed a much better selectivity and a single of these compounds showed even better antiplasmodial activity and selectivity than chloroquine.
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1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Alcanos
/
Antiprotozoários
Limite:
Animals
Idioma:
En
Revista:
Eur J Med Chem
Ano de publicação:
2010
Tipo de documento:
Article