Síntesis, caracterización y evaluación antimicrobiana in vitro de derivados de sulfonilurea como inhibidores potenciales de la beta-cetoacil-proteína portadora de acilo III sintasa (FabH)
Vol. 25 Núm. 1 (2015), Artículos
Vol. 25 Núm. 1 (2015)

Síntesis, caracterización y evaluación antimicrobiana in vitro de derivados de sulfonilurea como inhibidores potenciales de la beta-cetoacil-proteína portadora de acilo III sintasa (FabH)

Artículos
https://doi.org/10.15174/au.2015.658
Publicado 2015-03-09
Aluru Raghavendra Guru Prasad
ICFAI Foundation for Higher Education, Sankarpally Road, Hyderabad, AP., India
Badampudi Santosh Kumar
Department of Chemistry, Sri Krishnadevaraya University, Anantapur, A.P., India.
Papammagari Raveendra Reddy
Sri Krishnadevaraya University, Anantapur, A.P., India.
Alvala Mallika
National Institute of Pharmaceutical Education and Research, Balanagar, Hyderabad.
Lakshmana Rao Krishna Rao Ravindranath
Sri Krishnadevaraya University, Anantapur, A.P., India.
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Palabras clave

Sintasa β-cetoacil-ACP III (FabH)
caracterización de derivados de sulfonilurea
actividad antimicrobiana
in vitro
in silico. β-ketoacyl-acyl carrier protein synthase III (FabH)
sulphonyl urea derivatives characterization
antimicrobial activity
in vitro
in silico.

Cómo citar

Guru Prasad, A. R., Santosh Kumar, B., Raveendra Reddy, P., Mallika, A., & Ravindranath, L. R. K. R. (2015). Síntesis, caracterización y evaluación antimicrobiana in vitro de derivados de sulfonilurea como inhibidores potenciales de la beta-cetoacil-proteína portadora de acilo III sintasa (FabH). Acta Universitaria, 25(1), 12–21. https://doi.org/10.15174/au.2015.658
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Resumen

Se sintetizó una serie de 15 derivados de sulfonilurea (7a-7o) que contiene diversos sustituyentes heterocíclicos, caracterizados por análisis elemental, IR, RMN de 1H y de 13C espectros RMN, y se evaluaron in vitro para actividad antibacteriana y antifúngica. Se realizaron estudios de acoplamiento molecular para calcular las puntuaciones de conexión y proponer el modo de unión de derivados de sulfonilurea con E. coli beta-cetoacil-ACP sintasa III, una enzima clave que cataliza la etapa inicial de la biosíntesis de ácidos grasos a través de un tipo II disociado ácido graso sintasa. Los resultados de este estudio revelaron que los derivados de 7 g, vj, 7l y 7o pueden convertirse en posibles moléculas de plomo para el descubrimiento de fármacos antimicrobianos. Los estudios in vitro confirmaron que los derivados de 7g, 7j, 7l y 7o han demostrado una mejor actividad antimicrobiana que los otros.

 
https://doi.org/10.15174/au.2015.658
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PDF (English)

Citas

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