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Your search keyword '"Oriana Tabarrini"' showing total 8 results
Start Over Author "Oriana Tabarrini" Publisher american chemical society
8 results on '"Oriana Tabarrini"'

1. [1,2,4]Triazolo[3,4-b]benzothiazole scaffold as versatile nicotinamide mimic allowing nanomolar inhibition of different PARP enzymes

Author

Sudarshan Murthy, Maria Giulia Nizi, Mirko M. Maksimainen, Serena Massari, Juho Alaviuhkola, Barbara E. Lippok, Chiara Vagaggini, Sven T. Sowa, Albert Galera-Prat, Yashwanth Ashok, Harikanth Venkannagari, Renata Prunskaite-Hyyryläinen, Elena Dreassi, Bernhard Lüscher, Patricia Korn, Oriana Tabarrini, and Lari Lehtiö

Subjects
Scaffolds, Inhibitors, Drug Discovery, Molecular Medicine, Reaction products, ddc:610, Peptides and proteins, Assays
Abstract

Journal of medicinal chemistry 66(2), 1301-1320 (2023). doi:10.1021/acs.jmedchem.2c01460, Published by American Chemical Society, Washington, DC

Published
2023
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2. Pharmacophore-Based Repositioning of Approved Drugs as Novel Staphylococcus aureus NorA Efflux Pump Inhibitors

Author

Violetta Cecchetti, Serena Massari, Glenn W. Kaatz, Andrea Astolfi, Giuseppe Manfroni, Maria Letizia Barreca, Donatella Pietrella, Nunzio Iraci, Tommaso Felicetti, Oriana Tabarrini, and Stefano Sabatini

Subjects
Models, Molecular, 0301 basic medicine, Staphylococcus aureus, In silico, 030106 microbiology, NorA efflux pump, Pharmacology, CIPROFLOXACIN, Antimicrobial resistance, Ligands, medicine.disease_cause, MECHANISMS, 03 medical and health sciences, Antibiotic resistance, Bacterial Proteins, Drug Discovery, medicine, Humans, FLUOROQUINOLONE RESISTANCE, Pharmacophore model, S. aureus, NorA efflux pump, Drug repositioning, Antimicrobial resistance, Chemistry, DERIVATIVES, POTENT, TRANSPORTER, Drug Repositioning, ANTIBIOTIC-RESISTANCE, Staphylococcal Infections, S. aureus, Ligand (biochemistry), Anti-Bacterial Agents, Drug repositioning, GENETICALLY RELATED STRAINS, 030104 developmental biology, BACTERIA, Pharmacophore model, Molecular Medicine, GENETICALLY RELATED STRAINS, FLUOROQUINOLONE RESISTANCE, ANTIBIOTIC-RESISTANCE, DERIVATIVES, BACTERIA, POTENT, PHENOTHIAZINES, CIPROFLOXACIN, TRANSPORTER, MECHANISMS, Efflux, PHENOTHIAZINES, Multidrug Resistance-Associated Proteins, Pharmacophore
Abstract

An intriguing opportunity to address antimicrobial resistance is represented by the inhibition of efflux pumps. Focusing on NorA, the most important efflux pump of Staphylococcus aureus, an efflux pump inhibitors (EPIs) library was used for ligand-based pharmacophore modeling studies. By exploitation of the obtained models, an in silico drug repositioning approach allowed for the identification of novel and potent NorA EPIs.

Published
2017

7. Structure−Activity Relationship Study on Anti-HIV 6-Desfluoroquinolones.

Author

Oriana Tabarrini, Serena Massari, Dirk Daelemans, Miguel Stevens, Giuseppe Manfroni, Stefano Sabatini, Jan Balzarini, Violetta Cecchetti, Christophe Pannecouque, and Arnaldo Fravolini

Subjects
*CELL culture, *MOLECULES, *CULTURES (Biology), *AIDS
Abstract

On the basis of our recent findings that 6-aminoquinolones inhibit the HIV Tat-mediated transactivation, we have designed a broad series of derivatives identifying novel potent agents such as the 6-desfluoroquinolones 24( HM12) and 27( HM13), which showed pronounced anti-HIV activity in acutely, chronically, and latently HIV-1 infected cell cultures. We demonstrate here that highly potent molecules can be obtained by optimizing the substituent in the various positions of the quinolone nucleus. [ABSTRACT FROM AUTHOR]

Published
2008
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