%0 Journal Article
%T Structure-Antibacterial Activity Relationships of N-Substituted-(d-/l-Alaninyl) 1H-1,2,3-Triazolylmethyl Oxazolidinones
%A Edet Ekpenyong Udo
%A Oludotun Adebayo Phillips
%A Roselyn Jennifer DĄ¯silva
%J -
%D 2018
%R https://doi.org/10.3390/scipharm86040042
%X Abstract Bacterial resistance towards the existing class of antibacterial drugs continues to increase, posing a significant threat to the clinical usefulness of these drugs. These increasing and alarming rates of antibacterial resistance development and the decline in the number of new antibacterial drugsĄ¯ approval continue to serve as a major impetus for research into the discovery and development of new antibacterial agents. We synthesized a series of d-/ l-alaninyl substituted triazolyl oxazolidinone derivatives and evaluated their antibacterial activity against selected standard Gram-positive and Gram-negative bacterial strains. Overall, the compounds showed moderate to strong antibacterial activity. Compounds 9d and 10d ( d- and l-alaninyl derivatives bearing the 3,5-dinitrobenzoyl substituent), 10e ( l-alaninyl derivative bearing the 5-nitrofurancarbonyl group) and 9f and 10f ( d- and l-alaninyl derivatives bearing the 5-nitrothiophene carbonyl moiety) demonstrated antibacterial activity (MIC: 2 ĻĖg/mL) against Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecalis and Moraxella catarrhalis standard bacterial strains. No significant differences were noticeable between the antibacterial activity of the d- and l-alaninyl derivatives as a result of the stereochemistry of the compounds. View Full-Tex
%K antibacterial
%K linezolid
%K SARs
%K alaninyl-oxazolidinone
%K triazolyl-oxazolidinone
%U https://www.mdpi.com/2218-0532/86/4/42