0000000000390934

AUTHOR

Roberta Listro

showing 2 related works from this author

Novel Sortase A Inhibitors to Counteract Gram-Positive Bacterial Biofilms

2019

Sortase A (SrtA) is a membrane enzyme responsible for the covalent anchoring of surface proteins on the cell wall of Gram-positive bacteria. Nowadays it is considered an interesting target for the development of new anti-infective drugs which aim to interfere with important Gram-positive virulence mechanisms. Along the years, we studied the anti-staphylococcal and anti-biofilm activity of some natural and synthetic polyhalogenated pyrrolic compounds, called pyrrolomycins. Some of them were active on Gram-positive pathogens at a μg/mL range of concentration (1.5-0.045 μg/mL) and showed a biofilm inhibition in the range of 50-80%. [1-3] In light of these encouraging results, herein we present…

chemistry.chemical_classificationbiologyGram-positive virulence mechanismsChemistrySortase ABiofilmlcsh:ASettore BIO/19 - Microbiologia Generalebiology.organism_classificationSettore CHIM/08 - Chimica FarmaceuticaCell wallAnti-infective drugsMembraneEnzymen/aSettore CHIM/03 - Chimica Generale E InorganicaCovalent bondSortase Amental disordersBiophysicslcsh:General WorksAnti-biofilm activityPyrrolomycinsBacteriaGramProceedings
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Pyrrolomycins as antimicrobial agents. Microwave-assisted organic synthesis and insights into their antimicrobial mechanism of action

2019

Abstract New compounds able to counteract staphylococcal biofilm formation are needed. In this study we investigate the mechanism of action of pyrrolomycins, whose potential as antimicrobial agents has been demonstrated. We performed a new efficient and easy method to use microwave organic synthesis suitable for obtaining pyrrolomycins in good yields and in suitable amount for their in vitro in-depth investigation. We evaluate the inhibitory activity towards Sortase A (SrtA), a transpeptidase responsible for covalent anchoring in Gram-positive peptidoglycan of many surface proteins involved in adhesion and in biofilm formation. All compounds show a good inhibitory activity toward SrtA, havi…

Staphylococcus aureusClinical BiochemistryPharmaceutical ScienceMicrobial Sensitivity Testsmedicine.disease_causeSettore BIO/19 - Microbiologia Generale01 natural sciencesBiochemistrychemistry.chemical_compoundBacterial ProteinsDrug DiscoverymedicinePyrrolesEnzyme InhibitorsMicrowavesMolecular BiologyEnzyme Assays010405 organic chemistryChemistryOrganic ChemistryBiofilmN-Acetylmuramoyl-L-alanine AmidaseAntimicrobialAminoacyltransferasesAntimicrobial resistance Pyrrolomycins Sortase A Staphylococcus aureus In-silico docking studies MAOS Pharmacokinetics studies Murein hydrolase activitySettore CHIM/08 - Chimica Farmaceutica0104 chemical sciencesAnti-Bacterial AgentsMolecular Docking Simulation010404 medicinal & biomolecular chemistryCysteine EndopeptidasesBiochemistryMechanism of actionDocking (molecular)Staphylococcus aureusSettore CHIM/03 - Chimica Generale E InorganicaSortase ABiofilmsPseudomonas aeruginosaMolecular MedicineOrganic synthesisPeptidoglycanmedicine.symptom
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