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Molecules 2018, 23(2), 284; https://doi.org/10.3390/molecules23020284

Overcoming Aminoglycoside Enzymatic Resistance: Design of Novel Antibiotics and Inhibitors

1
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
2
Facultad de Ciencias Químico Farmacéuticas y Bioquímicas, Universidad Mayor Real y Pontificia de San Francisco Xavier de Chuquisaca, Dalence 51, Casilla 497, Sucre, Bolivia
3
Departmento de Química Bio-Orgánica, Instituto de Química Orgánica General (CSIC), Juan de la Cierva 3, 28006 Madrid, Spain
*
Authors to whom correspondence should be addressed.
Received: 7 November 2017 / Revised: 12 January 2018 / Accepted: 26 January 2018 / Published: 30 January 2018
(This article belongs to the Special Issue Recent Development on the New Applications of Aminoglycosides)
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Abstract

Resistance to aminoglycoside antibiotics has had a profound impact on clinical practice. Despite their powerful bactericidal activity, aminoglycosides were one of the first groups of antibiotics to meet the challenge of resistance. The most prevalent source of clinically relevant resistance against these therapeutics is conferred by the enzymatic modification of the antibiotic. Therefore, a deeper knowledge of the aminoglycoside-modifying enzymes and their interactions with the antibiotics and solvent is of paramount importance in order to facilitate the design of more effective and potent inhibitors and/or novel semisynthetic aminoglycosides that are not susceptible to modifying enzymes. View Full-Text
Keywords: antibiotic resistance; combination therapy; bi-substrate inhibitors; decoy acceptors antibiotic resistance; combination therapy; bi-substrate inhibitors; decoy acceptors
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Zárate, S.G.; De la Cruz Claure, M.L.; Benito-Arenas, R.; Revuelta, J.; Santana, A.G.; Bastida, A. Overcoming Aminoglycoside Enzymatic Resistance: Design of Novel Antibiotics and Inhibitors. Molecules 2018, 23, 284.

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