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|Title:||Research on anti-HIV-1 agents. Part 2. Solid-phase synthesis, biological evaluation and molecular modeling studies of 2,5,6-trisubstituted-4(3H)-pyrimidinones targeting HIV-1 reverse transcriptase||Authors:||Botta, Maurizio
A small library of 2,6-disubstituted- and 2,5,6-trisubstituted-4(3H)-pyrimidinones has been synthesized by solid-phase synthesis starting from a modified Merrifield resin. The new pyrimidinones have been tested in vitro for their ability to inhibit HIV-1 RT in comparison with nevirapine. Interestingly, some of them showed moderate activity against recombinant RTs carrying mutations conferring resistance to TIBO/nevirapine. The possible mode of binding between Y188L mutant of RT and the new compounds has been studied through a molecular modeling approach.
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