Dithiocarbamates effectively inhibit the alpha-carbonic anhydrase from Neisseria gonorrhoeae

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dc.contributor.authorGiovannuzzi, Simoneen
dc.contributor.authorAbutaleb, Nader S.en
dc.contributor.authorHewitt, Chad S.en
dc.contributor.authorCarta, Fabrizioen
dc.contributor.authorNocentini, Alessioen
dc.contributor.authorSeleem, Mohamed N.en
dc.contributor.authorFlaherty, Daniel P.en
dc.contributor.authorSupuran, Claudiu T.en
dc.date.accessioned2022-08-24T17:13:04Zen
dc.date.available2022-08-24T17:13:04Zen
dc.date.issued2022-01-01en
dc.description.abstractRecently, inorganic anions and sulphonamides, two of the main classes of zinc-binding carbonic anhydrase inhibitors (CAIs), were investigated for inhibition of the alpha-class carbonic anhydrase (CA, EC 4.2.1.1) from Neisseria gonorrhoeae, NgCA. As an extension to our previous studies, we report that dithiocarbamates (DTCs) derived from primary or secondary amines constitute a class of efficient inhibitors of NgCA. K(I)s ranging between 83.7 and 827 nM were measured for a series of 31 DTCs that incorporated various aliphatic, aromatic, and heterocyclic scaffolds. A subset of DTCs were selected for antimicrobial testing against N. gonorrhoeae, and three molecules displayed minimum inhibitory concentration (MIC) values less than or equal to 8 mu g/mL. As NgCA was recently validated as an antibacterial drug target, the DTCs may lead to development of novel antigonococcal agents.en
dc.description.notesCTS thank the Italian Ministry for University and Research (MIUR), project FISR2019_04819 BacCAD. The research program was partially funded by a Purdue Institute for Drug Discovery Programmatic Grant (to M.N.S. and D.P.F.) and NIH/NIAID 1R01AI148523 (to M.N.S and D.P.F.). Fabrizio Carta (F~C.) is grateful to "Bando di Ateneo per il Finanziamento di Progetti Competitivi per Ricercatori a Tempo Determinato (RTD) dell'Universita di Firenze" 2020-202100, and Fondazione Cassa di Risparmio di Firenze (Grant Number ECR2018.1001) for partially supporting this work.en
dc.description.sponsorshipItalian Ministry for University and Research (MIUR) [FISR2019_04819 BacCAD]; Purdue Institute for Drug Discovery Programmatic Grant; NIH/NIAID [1R01AI148523]; Fondazione Cassa di Risparmio di Firenze [ECR2018.1001]; "Bando di Ateneo per il Finanziamento di Progetti Competitivi per Ricercatori a Tempo Determinato (RTD) dell'Universita di Firenze" [2020-202100]en
dc.description.versionPublished versionen
dc.format.mimetypeapplication/pdfen
dc.identifier.doihttps://doi.org/10.1080/14756366.2021.1988945en
dc.identifier.eissn1475-6374en
dc.identifier.issn1475-6366en
dc.identifier.issue1en
dc.identifier.pmid34894954en
dc.identifier.urihttp://hdl.handle.net/10919/111622en
dc.identifier.volume37en
dc.language.isoenen
dc.publisherTaylor & Francisen
dc.rightsCreative Commons Attribution 4.0 Internationalen
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/en
dc.subjectCarbonic anhydraseen
dc.subjectinhibitoren
dc.subjectdithiocarbamateen
dc.subjectNeisseria gonorrhoeaeen
dc.subjectantibacterialsen
dc.titleDithiocarbamates effectively inhibit the alpha-carbonic anhydrase from Neisseria gonorrhoeaeen
dc.title.serialJournal of Enzyme Inhibition and Medicinal Chemistryen
dc.typeArticle - Refereeden
dc.type.dcmitypeTexten

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