Since their discovery in 1992,3,4-dihydro-2-alkoxy-6-benzyl-4- oxypyrimidines (DABOs) have been subjected to many structural modifications in order to obtain better non-nucleoside reverse transcriptase inhibitors (NNRTIs) for the treatment of AIDS. Herein, we report a straightforward and versatile route for the synthesis of novel C-6 arylmethyl-functionalized S-DABO, a poorly explored class of derivatives. Finally, biological evaluation of the synthesized derivatives led to the identification of a promising anti-HIV-1 lead compound.
A Versatile Route to C-6 Arylmethyl-FunctionalizedS-DABO and Related Analogues / Radi, Marco; Lorenzo, Contemori; Daniele, Castagnolo; Raffaella, Spinosa; José A., Esté; Silvio, Massa; Maurizio, Botta. - In: ORGANIC LETTERS. - ISSN 1523-7060. - 9:(2007), pp. 3157-3160. [10.1021/ol071225i]
A Versatile Route to C-6 Arylmethyl-FunctionalizedS-DABO and Related Analogues
RADI, Marco;
2007-01-01
Abstract
Since their discovery in 1992,3,4-dihydro-2-alkoxy-6-benzyl-4- oxypyrimidines (DABOs) have been subjected to many structural modifications in order to obtain better non-nucleoside reverse transcriptase inhibitors (NNRTIs) for the treatment of AIDS. Herein, we report a straightforward and versatile route for the synthesis of novel C-6 arylmethyl-functionalized S-DABO, a poorly explored class of derivatives. Finally, biological evaluation of the synthesized derivatives led to the identification of a promising anti-HIV-1 lead compound.| File | Dimensione | Formato | |
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