Publication: Síntesis quimioenzimática para la obtención de compuestos antiinfecciosos
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2015-07
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Abstract
Desde el descubrimiento de la penicilina, se han venido produciendo numerosos antibióticos para el tratamiento de distintas enfermedades infecciosas, y gracias a ello se ha modificado favorablemente el panorama de la morbilidad y mortalidad ya que estas afecciones ocupan el primer lugar entre las causas de muerte.
En estos últimos años, el uso de las enzimas en las industrias farmacéuticas se ha incrementado por la excelente selectividad (regio- quimio- y estereoselectividad) que presentan los biocatalizadores y la buena sostenibilidad que nos proporciona su empleo, permitiéndonos obtener productos semisintéticos difícilmente alcanzables por los métodos químicos clásicos.
El presente artículo se divide en 3 partes. En primer lugar, se describen los mecanismos de acción de las principales familias de fármacos con actividad antibacteriana. En segundo lugar, se indican varias de las ventajas que posee el uso de la biocatálisis para la síntesis de compuestos con fines terapéuticos. Por último, se detalla la semisíntesis de los β-lactámicos, describiendo como se obtienen los productos intermediarios como 6-APA, 7-ADCA y 7-ACA y comparando su obtención a través de reacciones químicas o por vías enzimáticas, utilizando como principal biocatalizador la penicilin G acilasa.
Since the discovery of penicillium, it has been producing so many antibiotics for the treatment of different infectious diseases, and thanks to that, it let change outlook of morbidity and mortality for better, where this illness occupy the first place among the causes of death. In the last years, the use of enzymes in the pharmaceutical industry has increased because of the excellent chemoselectivity (regio and stereoselectivity) of biocatalyst, and the good sustainability that provide us its employment, allowing us to get semisynthetic products hardly achievable by classics chemical methods. In this article, it divides in three parts. First of all, it describes the mechanism of action of the principles groups of drugs with antibacterial activity. In second place, it explains and formulates several advantages that the employment of biocatalyst has for the synthesis of compounds for therapeutic aims. Finally, it details the semisynthesis of β-lactams, describing how to obtain the intermediates products like 6-APA, 7-ADCA and 7-ACA, and comparing their obtaining through chemicals reactions or enzymatically, using the principal biocatalyst penicillin G acylase.
Since the discovery of penicillium, it has been producing so many antibiotics for the treatment of different infectious diseases, and thanks to that, it let change outlook of morbidity and mortality for better, where this illness occupy the first place among the causes of death. In the last years, the use of enzymes in the pharmaceutical industry has increased because of the excellent chemoselectivity (regio and stereoselectivity) of biocatalyst, and the good sustainability that provide us its employment, allowing us to get semisynthetic products hardly achievable by classics chemical methods. In this article, it divides in three parts. First of all, it describes the mechanism of action of the principles groups of drugs with antibacterial activity. In second place, it explains and formulates several advantages that the employment of biocatalyst has for the synthesis of compounds for therapeutic aims. Finally, it details the semisynthesis of β-lactams, describing how to obtain the intermediates products like 6-APA, 7-ADCA and 7-ACA, and comparing their obtaining through chemicals reactions or enzymatically, using the principal biocatalyst penicillin G acylase.