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

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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Bibliographic Details
Main Authors: Graziella Tocco, Francesca Esposito, Pierluigi Caboni, Antonio Laus, John A. Beutler, Jennifer A. Wilson, Angela Corona, Stuart F. J. Le Grice, Enzo Tramontano
Format: Article
Language:English
Published: Taylor & Francis Group 2020-01-01
Series:Journal of Enzyme Inhibition and Medicinal Chemistry
Subjects:
bioisosters
rnase h allosteric inhibitors
hiv-1 virus
rnase h
integrase
Online Access:http://dx.doi.org/10.1080/14756366.2020.1835884

Internet

http://dx.doi.org/10.1080/14756366.2020.1835884

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