A series of new AZT conjugates with alkyl and oxyalkyl ether phospholipids was synthesized and evaluated for inhibitory activities against HIV-1 and HIV-2. The alkoxyethyl derivatives 6a-c proved 3- to 5-fold more active against HIV-1 and HIV-2 than the alkyl analogues 6d-f. A trend for higher activity with longer alkyl side-chains was observed. However, the analogues with the shortest chain possessed the most favourable therapeutic index.
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Calogeropoulou et al. (1995) studied this question.
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