Synthesis, characterization and in vitro antimicrobial evaluation of sulphonyl urea derivatives as potential inhibitors of beta-ketoacyl-acyl carrier protein synthase III (FabH)
Vol. 25 No. 1 (2015), Artículos
Vol. 25 No. 1 (2015)

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

Artículos
https://doi.org/10.15174/au.2015.658
Published 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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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
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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. 

https://doi.org/10.15174/au.2015.658
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