Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10595809 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
Abstract
We report in this work the preparation and in vitro antimicrobial evaluation of novel amphiphilic aromatic amino alcohols synthesized by reductive amination of 4-alkyloxybenzaldehyde with 2-amino-2-hydroxymethyl-propane-1,3-diol. The antibacterial activity was determined against four standard strains (Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Pseudomonas aeruginosa) and 21 clinical isolates of methicillin-resistant Staphylococcus aureus. The antifungal activity was evaluated against four yeast (Candida albicans, Candida tropicalis, Candida glabrata and Candida parapsilosis). The results obtained showed a strong positive correlation between the lipophilicity and the antibiotic activity of the tested compounds. The best activities were obtained against the Gram-positive bacteria (MIC = 2-16 μg mlâ1) for the five compounds bearing longer alkyl chains (4c-g; 8-14 carbons), which were also the most active against Candida (MIC = 2-64 μg mlâ1). Compound 4e exhibited the highest levels of inhibitory activity (MIC = 2-16 μg mlâ1) against clinical isolates of MRSA. A concentration of twice the MIC resulted in bactericidal activity of 4d against 19 of the 21 clinical isolates.
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Chemistry
Organic Chemistry
Authors
Angelina M. de Almeida, Thiago Nascimento, Bianca S. Ferreira, Pedro P. de Castro, Vânia L. Silva, Claúdio G. Diniz, Mireille Le Hyaric,