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Volume 8
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10.3390/antibiotics8030109
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Article

Synthesis of Ring II/III Fragment of Kanamycin: A New Minimum Structural Motif for Aminoglycoside Recognition

by
Sandra G. Zárate
1,2,
Agatha Bastida
1,
Andrés G. Santana
1,* and
Julia Revuelta
1,*
1
Instituto de Química Orgánica General, CSIC, Juan de la Cierva 3, 28006 Madrid, Spain
2
Facultad de Tecnología, Carrera de Ingeniería Química, Universidad Mayor, Real y Pontificia de San Francisco Xavier de Chuquisaca, Regimiento Campos 180, Casilla 60-B Sucre, Bolivia
*
Authors to whom correspondence should be addressed.
Antibiotics 2019, 8(3), 109; https://doi.org/10.3390/antibiotics8030109
Submission received: 19 June 2019 / Revised: 25 July 2019 / Accepted: 31 July 2019 / Published: 2 August 2019
(This article belongs to the Special Issue Chemical Tools for Antibiotics Research)
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Abstract

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.
Keywords: aminoglycoside antibiotics; enzymatic resistance; minimum structural motif; oligosaccharides; pseudo-disaccharide aminoglycoside antibiotics; enzymatic resistance; minimum structural motif; oligosaccharides; pseudo-disaccharide
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MDPI and ACS Style

Zárate, S.G.; Bastida, A.; Santana, A.G.; Revuelta, J. Synthesis of Ring II/III Fragment of Kanamycin: A New Minimum Structural Motif for Aminoglycoside Recognition. Antibiotics 2019, 8, 109. https://doi.org/10.3390/antibiotics8030109

AMA Style

Zárate SG, Bastida A, Santana AG, Revuelta J. Synthesis of Ring II/III Fragment of Kanamycin: A New Minimum Structural Motif for Aminoglycoside Recognition. Antibiotics. 2019; 8(3):109. https://doi.org/10.3390/antibiotics8030109

Chicago/Turabian Style

Zárate, Sandra G., Agatha Bastida, Andrés G. Santana, and Julia Revuelta. 2019. "Synthesis of Ring II/III Fragment of Kanamycin: A New Minimum Structural Motif for Aminoglycoside Recognition" Antibiotics 8, no. 3: 109. https://doi.org/10.3390/antibiotics8030109

APA Style

Zárate, S. G., Bastida, A., Santana, A. G., & Revuelta, J. (2019). Synthesis of Ring II/III Fragment of Kanamycin: A New Minimum Structural Motif for Aminoglycoside Recognition. Antibiotics, 8(3), 109. https://doi.org/10.3390/antibiotics8030109

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