Tetrahedron

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 …

…, F Corelli, G Maga, F Manetti, M Renzulli, S Spadari

Index: Botta, Maurizio; Corelli, Federico; Maga, Giovanni; Manetti, Fabrizio; Renzulli, Michela; Spadari, Silvio Tetrahedron, 2001 , vol. 57, # 39 p. 8357 - 8367

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Citation Number: 49

Abstract

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 ...