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(16), 3157-3160 [10.1021/ol071225i].
A Versatile Route to C-6 Arylmethyl-Functionalized S-DABO and Related Analogues
Botta, Maurizio;Contemori, Lorenzo;Castagnolo, Daniele;Spinosa, Raffaella;Massa, Silvio;Botta, M.
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.
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https://hdl.handle.net/11365/21102
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