European Journal of Medicinal Chemistry p. 935 - 949 (2001)
Update date:2022-08-05
Topics:
Di Braccio, Mario
Grossi, Giancarlo
Roma, Giorgio
Vargiu, Laura
Mura, Massimo
Marongiu, Maria Elena
A number of properly substituted 5H-pyrimido[4,5-b][1,5]benzodiazepines (2) and pyrazolo[3,4-b][1,5]benzodiazepines (3 and 4), as well as compounds 5-7, which are derivatives of new tetracyclic systems, were prepared as nevirapine analogues through multistep synthetic routes. The cytotoxic and anti-HIV-1 properties of compounds 2-7 were evaluated in cell-based assays, together with their inhibitory activity against the HIV-1 recombinant reverse transcriptase (rRT) in enzyme assays. The modifications introduced into nevirapine heterocyclic skeleton proved to have a negative effect for the anti-HIV-1 activity. It is worth noting that some of the new derivatives proved to be cytotoxic in the low micromolar range.
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Doi:10.1016/S0022-2860(01)00811-0
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