SYNTHESIS AND ANTI-HIV EVALUATION OF ALKYL AND ALKOXYETHYL PHOSPHODIESTER AZT DERIVATIVES

Authors
CALOGEROPOULOU T KOUFAKI M TSOTINIS A BALZARINI J DECLERCQ E MAKRIYANNIS A
Citation
T. Calogeropoulou et al., SYNTHESIS AND ANTI-HIV EVALUATION OF ALKYL AND ALKOXYETHYL PHOSPHODIESTER AZT DERIVATIVES, Antiviral chemistry & chemotherapy, 6(1), 1995, pp. 43-49
Citations number
32
Categorie Soggetti
Biology,"Pharmacology & Pharmacy
Journal title
Antiviral chemistry & chemotherapy → ACNP
ISSN journal
09563202
Volume
6
Issue
1
Year of publication
1995
Pages
43 - 49
Database
ISI
SICI code
0956-3202(1995)6:1<43:SAAEOA>2.0.ZU;2-5
Abstract
A series of new AZT conjugates with alkyl and oxyalkyl ether phospholi pids was synthesized and evaluated for inhibitory activities against H IV-1 and HIV-2. The alkoxyethyl derivatives 6a-c proved 3- to 5-fold m ore active against HIV-1 and H1V-2 than the alkyl analogues 6d-f. A tr end for higher activity with longer alkyl side-chains was observed. Ho wever, the analogues with the shortest chain possessed the most favour able therapeutic index.