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Start Over Author "Marco Piccoli" Publisher elsevier bv
3 results on '"Marco Piccoli"'

2. PO-02-146 MULTI-OMICS ANALYSIS REVEALS THE METABOLIC AND POLYGENIC BASIS OF BRUGADA SYNDROME

Author

Carlo Pappone, Giuseppe Ciconte, Vladimir Espinosa Angarica, Andrea Ghiroldi, Emanuele Micaglio, Pasquale Creo, Adriana Tarantino, Michelle Monasky, Marco Piccoli, Flavio Mastrocinque, Sara D'Imperio, Zarko Calovic, Antonio Boccellino, Federica Cirillo, Lorenzo Menicanti, Fiorenzo Gaita, Gabriele Vicedomini, Vincenzo Santinelli, Enrico Petretto, and Luigi Anastasia

Subjects
Physiology (medical), Cardiology and Cardiovascular Medicine
Published
2023
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3. 2β-3,4-Unsaturated sialic acid derivatives: Synthesis optimization, and biological evaluation as Newcastle disease virus hemagglutinin-neuraminidase inhibitors

Author

Luigi Anastasia, Paola Rota, Pietro Allevi, Federica Cirillo, Paolo La Rocca, Marco Piccoli, Andrea Ghiroldi, and Valentina Franco

Subjects
Glycosylation, Clinical Biochemistry, Newcastle disease virus, Neuraminidase, Pharmaceutical Science, Sialidase, Antiviral Agents, Biochemistry, Structure-Activity Relationship, chemistry.chemical_compound, Hydrolysis, Drug Discovery, Humans, Enzyme Inhibitors, Molecular Biology, IC50, Dose-Response Relationship, Drug, Molecular Structure, biology, Organic Chemistry, Active site, Sialic acid, Hemagglutinins, chemistry, Acetylation, Sialic Acids, biology.protein, Molecular Medicine, Hemagglutinin-neuraminidase
Abstract

The optimization of the synthetic protocol to obtain the 3,4-unsaturated sialic acid derivatives, through the fine-tuning of both the Ferrier glycosylation conditions and the subsequent hydrolysis work-up, is herein reported. The accomplishment of the desired β-anomers and some selected α-ones, in pure form, led us to evaluate their specific inhibitory activity towards NDV-HN and human sialidase NEU3. Importantly, the resulting data allowed the identification, for the first time, of three active 3,4-unsaturated sialic acid analogs, showing IC50 values against NDV-HN in the micromolar range.

Published
2020
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