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.
Botta, M., Contemori, L., Castagnolo, D., Spinosa, R., Este, J.A., Massa, S., et al. (2007). A Versatile Route to C-6 Arylmethyl-Functionalized S-DABO and Related Analogues. ORGANIC LETTERS, 9, 3157-3160.
A Versatile Route to C-6 Arylmethyl-Functionalized S-DABO and Related Analogues.
BOTTA, MAURIZIO;CONTEMORI, LORENZO;CASTAGNOLO, DANIELE;SPINOSA, RAFFAELLA;MASSA, SILVIO;
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 | |
|---|---|---|---|
|
ol071225i.pdf
non disponibili
Tipologia:
Post-print
Licenza:
NON PUBBLICO - Accesso privato/ristretto
Dimensione
99.6 kB
Formato
Adobe PDF
|
99.6 kB | Adobe PDF | Visualizza/Apri Richiedi una copia |
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
https://hdl.handle.net/11365/21102
Attenzione
Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo