1887

Abstract

A homologous series of 1-alkyl-(,-dimethylamino)pyridinium bromides, termed compounds 1–11, was synthesized and studied for antibacterial and antifungal activity. Of these, compound 8, containing a ten-carbon alkyl chain, showed maximum inhibition against all the tested bacterial strains. The highest antibacterial activity using a disc diffusion method was recorded against [zone of inhibition (ZOI): 45.75±0.25 mm], followed by , , , and . In addition to antibacterial activity, compounds 3–11 displayed good inhibitory action against the human opportunistic yeast pathogens and various spp. The maximum ZOI was observed against (51.5±0.5 mm) using compound 8, with ZOIs of 23.5±0.5, 32.0±0.0, 27.75±0.25 and 41.5±0.5 mm against , , and , respectively. Furthermore, compound 8 caused inhibition of the candidal yeast–hyphae transition at a concentration of 0.29 µM and also inhibited the secretion of extracellular hydrolytic enzyme such as secreted aspartyl proteinase at subinhibitory concentrations. Compound 8 showed very little haemolytic activity at a concentration of 0.58 µM (1.315±0.75 %), with its highest haemolytic activity (47.806±2.32 %) observed at a concentration of 2.9 µM.

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2013-02-01
2019-12-08
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