Discovery of novel fragments inhibiting O-acetylserine sulphhydrylase by combining scaffold hopping and ligand–based drug design

Discovery of novel fragments inhibiting O-acetylserine sulphhydrylase by combining scaffold hopping and ligand–based drug design

Several bacteria rely on the reductive sulphur assimilation pathway, absent in mammals, to synthesise cysteine. Reduction of virulence and decrease in antibiotic resistance have already been associated with mutations on the genes that codify cysteine biosynthetic enzymes. Therefore, inhibition of cy...

Description complète

Détails bibliographiques
Auteurs principaux: Joana Magalhães, Nina Franko, Giannamaria Annunziato, Martin Welch, Stephen K. Dolan, Agostino Bruno, Andrea Mozzarelli, Stefano Armao, Aigars Jirgensons, Marco Pieroni, Gabriele Costantino, Barbara Campanini
Format: Article
Langue:English
Publié: Taylor & Francis Group 2018-01-01
Collection:Journal of Enzyme Inhibition and Medicinal Chemistry
Sujets:
Scaffold hopping
fragments
O-acetylserine sulphhydrylase
medicinal chemistry
pyrazoles
ligand-based drug design
Accès en ligne:http://dx.doi.org/10.1080/14756366.2018.1512596

Internet

http://dx.doi.org/10.1080/14756366.2018.1512596

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