Vol. 25 No. 1 (2015)
Artículos de Investigación

Synthesis, characterization and in vitro antimicrobial evaluation of sulphonyl urea derivatives as potential inhibitors of beta-ketoacyl-acyl carrier protein synthase III (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

Published 2015-03-09

Keywords

  • 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.

How to Cite

Guru Prasad, A. R., Santosh Kumar, B., Raveendra Reddy, P., Mallika, A., & Ravindranath, L. R. K. R. (2015). Synthesis, characterization and in vitro antimicrobial evaluation of sulphonyl urea derivatives as potential inhibitors of beta-ketoacyl-acyl carrier protein synthase III (FabH). Acta Universitaria, 25(1), 12–21. https://doi.org/10.15174/au.2015.658

Abstract

A series of 15 sulphonyl urea derivatives (7a-7o) containing various heterocyclic substituents were synthesized, characterized by elemental analysis, IR, 1H NMR and 13C NMR spectra and evaluated for in vitro antibacterial and antifungal activity. Molecular docking studies were performed to calculate docking scores and to propose the binding mode of sulphonyl urea derivatives with E. coli beta-ketoacyl-acp synthase III, a key enzyme that catalyzes the initial step of fatty acid biosynthesis via a type II dissociated fatty acid synthase. The results from this study revealed that the derivatives 7g, vj, 7l and 7o can become possible lead molecules for antimicrobial drug discovery. In vitro antimicrobial studies confirmed that the derivatives 7g, 7j, 7l and 7o have demonstrated better activity than the others. 

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