Synthesis of 4-amino-5-cyano-2, 6-disubstituted pyrimidines as a potential antifilarial DNA topoisomerase II inhibitors.
Med Chem
; 4(6): 577-85, 2008 Nov.
Article
em En
| MEDLINE
| ID: mdl-18991743
ABSTRACT
A novel series of 4-amino-5-cyano-2, 6-disubstituted pyrimidines have been synthesized and evaluated for their in vitro antifilarial DNA topoisomerase II activity against filarial parasite Setaria Cervi. In particular compounds bearing 4-chloro-phenyl substitutent at position-6, exhibited strong inhibition at 40 microg/mL and 5 microg/mL concentration. The present study based on the biological results obtained, suggests that the nature of substitutent at position-4 in the phenyl ring directly affects DNA topoisomerase II inhibitory activity. Most of the compounds have shown better topoisomerase II inhibitory activity than the standard antifilarial drug (DEC) and the topoisomerase II inhibitors (Novobiocin, Nalidixic acid).
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Base de dados:
MEDLINE
Assunto principal:
Pirimidinas
/
Setaria (Nematoide)
/
Inibidores da Topoisomerase II
/
Filaricidas
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article