Abstract

SANTOSH KUMAR, Badampudi et al. Synthesis, characterization and in vitro santimicrobial evaluation of sulphonyl urea derivatives as potential inhibitors of beta-ketoacyl-acyl carrier protein synthase III (FabH). Acta univ [online]. 2015, vol.25, n.1, pp.12-21. ISSN 2007-9621.  https://doi.org/10.15174/au.2014.658.

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.

Keywords : β-ketoacyl-acyl carrier protein synthase III (FabH); sulphonyl urea derivatives characterization; antimicrobial activity; in vitro; in silico.

        · abstract in Spanish     · text in English     · English ( pdf )