Vol. 25 Núm. 1 (2015)
Artículos de Investigación

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)

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  • Aluru Raghavendra Guru Prasad,
  • Badampudi Santosh Kumar,
  • Papammagari Raveendra Reddy,
  • Alvala Mallika,
  • Lakshmana Rao Krishna Rao Ravindranath
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.
DOI: https://doi.org/10.15174/au.2015.658

Publicado 2015-03-09

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

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.

 
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