Scaffold hopping and optimisation of 3',4'-dihydroxyphenyl- containing thienopyrimidinones: synthesis of quinazolinone derivatives as novel allosteric inhibitors of HIV-1 reverse transcriptase-associated ribonuclease H

• Main Authors: Graziella Tocco (Author), Francesca Esposito (Author), Pierluigi Caboni (Author), Antonio Laus (Author), John A. Beutler (Author), Jennifer A. Wilson (Author), Angela Corona (Author), Stuart F. J. Le Grice (Author), Enzo Tramontano (Author)
• Format: Book
• Published: Taylor & Francis Group, 2020-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Bioisosteric replacement and scaffold hopping are powerful strategies in drug design useful for rationally modifying a hit compound towards novel lead therapeutic agents. Recently, we reported a series of thienopyrimidinones that compromise dynamics at the p66/p51 HIV-1 reverse transcriptase (RT)-as...