Synthesis of Ring II/III Fragment of Kanamycin: A New Minimum Structural Motif for Aminoglycoside Recognition
A novel protocol has been established to prepare the kanamycin ring II/III fragment, which has been validated as a minimum structural motif for the development of new aminoglycosides on the basis of its bactericidal activity even against resistant strains. Furthermore, its ability to act as a AAC-(6...
| Main Authors: | , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2019-08-01
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| Series: | Antibiotics |
| Subjects: | |
| Online Access: | https://www.mdpi.com/2079-6382/8/3/109 |
| _version_ | 1828425936960225280 |
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| author | Sandra G. Zárate Agatha Bastida Andrés G. Santana Julia Revuelta |
| author_facet | Sandra G. Zárate Agatha Bastida Andrés G. Santana Julia Revuelta |
| author_sort | Sandra G. Zárate |
| collection | DOAJ |
| description | A novel protocol has been established to prepare the kanamycin ring II/III fragment, which has been validated as a minimum structural motif for the development of new aminoglycosides on the basis of its bactericidal activity even against resistant strains. Furthermore, its ability to act as a AAC-(6′) and APH-(3′) binder, and as a poor substrate for the ravenous ANT-(4′), makes it an excellent candidate for the design of inhibitors of these aminoglycoside modifying enzymes. |
| first_indexed | 2024-12-10T16:38:41Z |
| format | Article |
| id | doaj.art-e2ba1a9fb32349b6a49082ed9c62ab07 |
| institution | Directory Open Access Journal |
| issn | 2079-6382 |
| language | English |
| last_indexed | 2024-12-10T16:38:41Z |
| publishDate | 2019-08-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Antibiotics |
| spelling | doaj.art-e2ba1a9fb32349b6a49082ed9c62ab072022-12-22T01:41:18ZengMDPI AGAntibiotics2079-63822019-08-018310910.3390/antibiotics8030109antibiotics8030109Synthesis of Ring II/III Fragment of Kanamycin: A New Minimum Structural Motif for Aminoglycoside RecognitionSandra G. Zárate0Agatha Bastida1Andrés G. Santana2Julia Revuelta3Instituto de Química Orgánica General, CSIC, Juan de la Cierva 3, 28006 Madrid, SpainInstituto de Química Orgánica General, CSIC, Juan de la Cierva 3, 28006 Madrid, SpainInstituto de Química Orgánica General, CSIC, Juan de la Cierva 3, 28006 Madrid, SpainInstituto de Química Orgánica General, CSIC, Juan de la Cierva 3, 28006 Madrid, SpainA novel protocol has been established to prepare the kanamycin ring II/III fragment, which has been validated as a minimum structural motif for the development of new aminoglycosides on the basis of its bactericidal activity even against resistant strains. Furthermore, its ability to act as a AAC-(6′) and APH-(3′) binder, and as a poor substrate for the ravenous ANT-(4′), makes it an excellent candidate for the design of inhibitors of these aminoglycoside modifying enzymes.https://www.mdpi.com/2079-6382/8/3/109aminoglycoside antibioticsenzymatic resistanceminimum structural motifoligosaccharidespseudo-disaccharide |
| spellingShingle | Sandra G. Zárate Agatha Bastida Andrés G. Santana Julia Revuelta Synthesis of Ring II/III Fragment of Kanamycin: A New Minimum Structural Motif for Aminoglycoside Recognition Antibiotics aminoglycoside antibiotics enzymatic resistance minimum structural motif oligosaccharides pseudo-disaccharide |
| title | Synthesis of Ring II/III Fragment of Kanamycin: A New Minimum Structural Motif for Aminoglycoside Recognition |
| title_full | Synthesis of Ring II/III Fragment of Kanamycin: A New Minimum Structural Motif for Aminoglycoside Recognition |
| title_fullStr | Synthesis of Ring II/III Fragment of Kanamycin: A New Minimum Structural Motif for Aminoglycoside Recognition |
| title_full_unstemmed | Synthesis of Ring II/III Fragment of Kanamycin: A New Minimum Structural Motif for Aminoglycoside Recognition |
| title_short | Synthesis of Ring II/III Fragment of Kanamycin: A New Minimum Structural Motif for Aminoglycoside Recognition |
| title_sort | synthesis of ring ii iii fragment of kanamycin a new minimum structural motif for aminoglycoside recognition |
| topic | aminoglycoside antibiotics enzymatic resistance minimum structural motif oligosaccharides pseudo-disaccharide |
| url | https://www.mdpi.com/2079-6382/8/3/109 |
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