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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

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...

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Detalles Bibliográficos
Autores principales: Tocco, Graziella, Esposito, Francesca, Caboni, Pierluigi, Laus, Antonio, Beutler, John A., Wilson, Jennifer A., Corona, Angela, Le Grice, Stuart F. J., Tramontano, Enzo
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7646544/
https://www.ncbi.nlm.nih.gov/pubmed/33143469
http://dx.doi.org/10.1080/14756366.2020.1835884