Antistaphylococcal Activity of Novel Salicylanilide Derivatives

Author(s): Annmarie Mollaghan, Jarmila Vinsova, Ales Imramovsky, Lesley Cotter, Brigid Lucey, Jim O'Mahony, Aisling Costelloe, Aidan Coffey.

Journal Name: Current Drug Discovery Technologies

Volume 9 , Issue 1 , 2012


This study examined the antibacterial properties of nineteen benzoxazole, isoniazid, ethionamide and salicylanilide derivatives against Staphylococcus aureus (S. aureus). It was found that three salicylanilide-derived compounds demonstrated antistaphylococcal activity: 5-Chloro-2-hydroxy-N-(4-(trifluoromethyl)phenyl)benzamide (5-Cl-4-CF3- SAL), 4-chloro-2-(3-chlorophenylcarbamyoyl)phenyl)-2-(benzyloxycarbonylamino)propanoate (AIM31) and 4-chloro-2- (4-(trifluoromethyl)phenylcarbamoyl)phenyl acetate (AIM33). Investigation of the chemical structures of these three compounds and comparison with a non-inhibitory salicylanilide compound (i.e. 5,3-diCl-SAL) illustrated that different combinations of chemical groups at defined positions on the salicylanilide core structure had a marked influence on antistaphylococcal activity. The most effective compound was AIM33 which inhibited staphylococcal growth and displayed an initial MIC value of 3.12 μg ml-1 and subsequent investigation revealed that an MIC as low as of 0.5 μg ml-1 was achievable. In this case, the dual presence of a trifluoromethyl group and an acetylated phenolic hydroxyl to the salicylanilide core structure led to greatly enhanced activity.

Keywords: Antimicrobial resistance, chemotherapeutic agents, MRSA, salicylanilide, Staphylococcus aureus, anti-staphylococcal drugs, Antistaphylococcal Activity, nosocomial pathogens, benzoxazole

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Article Details

Year: 2012
Page: [39 - 47]
Pages: 9
DOI: 10.2174/157016312799304525

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