Carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani chagasi are inhibited by benzoxaboroles
A series of 6-substituted ureido- and thioureido-benzoxaboroles were investigated as inhibitors of carbonic anhydrases from Trypanosoma cruzi (TcCA), and Leishmania donovani chagasi (LdcCA). Both enzymes were inhibited by benzoxaboroles in the micromolar range. Preferential inhibitory potency agains...
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2018-01-01
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| Series: | Journal of Enzyme Inhibition and Medicinal Chemistry |
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| Online Access: | http://dx.doi.org/10.1080/14756366.2017.1414808 |
| _version_ | 1830084149360197632 |
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| author | Alessio Nocentini Roberta Cadoni Pascal Dumy Claudiu T. Supuran Jean-Yves Winum |
| author_facet | Alessio Nocentini Roberta Cadoni Pascal Dumy Claudiu T. Supuran Jean-Yves Winum |
| author_sort | Alessio Nocentini |
| collection | DOAJ |
| description | A series of 6-substituted ureido- and thioureido-benzoxaboroles were investigated as inhibitors of carbonic anhydrases from Trypanosoma cruzi (TcCA), and Leishmania donovani chagasi (LdcCA). Both enzymes were inhibited by benzoxaboroles in the micromolar range. Preferential inhibitory potency against the β-CA LdcCA versus the α-CA TcCA was observed with submicromolar inhibitory activities. Some derivatives displayed excellent inhibitory and selectivity profile over the ubiquitous and physiological relevant human off-target hCA II. This study provides a convincing opportunity to study benzoxaborole scaffold for the design of antiprotozoan potential drugs targeting the pathogen’s carbonic anhydrases. |
| first_indexed | 2024-12-14T16:36:14Z |
| format | Article |
| id | doaj.art-afb6c0f671954c0c8af8e0bdd129ac30 |
| institution | Directory Open Access Journal |
| issn | 1475-6366 1475-6374 |
| language | English |
| last_indexed | 2024-12-14T16:36:14Z |
| publishDate | 2018-01-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Journal of Enzyme Inhibition and Medicinal Chemistry |
| spelling | doaj.art-afb6c0f671954c0c8af8e0bdd129ac302022-12-21T22:54:27ZengTaylor & Francis GroupJournal of Enzyme Inhibition and Medicinal Chemistry1475-63661475-63742018-01-0133128628910.1080/14756366.2017.14148081414808Carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani chagasi are inhibited by benzoxaborolesAlessio Nocentini0Roberta Cadoni1Pascal Dumy2Claudiu T. Supuran3Jean-Yves Winum4Institut des Biomolécules Max Mousseron (IBMM), UMR 5247 CNRS, ENSCM, Université de MontpellierInstitut des Biomolécules Max Mousseron (IBMM), UMR 5247 CNRS, ENSCM, Université de MontpellierInstitut des Biomolécules Max Mousseron (IBMM), UMR 5247 CNRS, ENSCM, Université de MontpellierUniversity of Florence, Polo ScientificoInstitut des Biomolécules Max Mousseron (IBMM), UMR 5247 CNRS, ENSCM, Université de MontpellierA series of 6-substituted ureido- and thioureido-benzoxaboroles were investigated as inhibitors of carbonic anhydrases from Trypanosoma cruzi (TcCA), and Leishmania donovani chagasi (LdcCA). Both enzymes were inhibited by benzoxaboroles in the micromolar range. Preferential inhibitory potency against the β-CA LdcCA versus the α-CA TcCA was observed with submicromolar inhibitory activities. Some derivatives displayed excellent inhibitory and selectivity profile over the ubiquitous and physiological relevant human off-target hCA II. This study provides a convincing opportunity to study benzoxaborole scaffold for the design of antiprotozoan potential drugs targeting the pathogen’s carbonic anhydrases.http://dx.doi.org/10.1080/14756366.2017.1414808BenzoxaboroleTrypanosoma cruziLeishmania donovani chagasiprotozoan carbonic anhydrasesinhibition |
| spellingShingle | Alessio Nocentini Roberta Cadoni Pascal Dumy Claudiu T. Supuran Jean-Yves Winum Carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani chagasi are inhibited by benzoxaboroles Journal of Enzyme Inhibition and Medicinal Chemistry Benzoxaborole Trypanosoma cruzi Leishmania donovani chagasi protozoan carbonic anhydrases inhibition |
| title | Carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani chagasi are inhibited by benzoxaboroles |
| title_full | Carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani chagasi are inhibited by benzoxaboroles |
| title_fullStr | Carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani chagasi are inhibited by benzoxaboroles |
| title_full_unstemmed | Carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani chagasi are inhibited by benzoxaboroles |
| title_short | Carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani chagasi are inhibited by benzoxaboroles |
| title_sort | carbonic anhydrases from trypanosoma cruzi and leishmania donovani chagasi are inhibited by benzoxaboroles |
| topic | Benzoxaborole Trypanosoma cruzi Leishmania donovani chagasi protozoan carbonic anhydrases inhibition |
| url | http://dx.doi.org/10.1080/14756366.2017.1414808 |
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