Synthesis and anti-HIV-1 activities of new pyrimido[5,4-b]indoles.
Farmaco
; 54(4): 255-64, 1999 Apr 30.
Article
em En
| MEDLINE
| ID: mdl-10384720
ABSTRACT
A set of new pyrimido[5,4-b]indole derivatives that are structurally related to some non-nucleside HIV-1 reverse transcriptase inhibitors were synthesized and biologically evaluated for their activity as inhibitors of wild and mutant HIV-1 RT types in an 'in vitro' recombinant HIV-1 RT screening assay, as well as anti-infectives in HLT4lacZ-1IIIB cells. Preliminary structure-activity relationships suggest that activity is promoted by simultaneous substitution in positions 2 and 4, especially when chains of alkyldiamine type are present, and by electron-releasing substituents (methoxy) in positions 7 and 8. The inactivity or the very low activity of title derivatives does not suggest interest in AIDS therapy.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
HIV-1
/
Inibidores da Transcriptase Reversa
/
Fármacos Anti-HIV
/
Indóis
Limite:
Humans
Idioma:
En
Revista:
Farmaco
Ano de publicação:
1999
Tipo de documento:
Article