4899-97-2Relevant articles and documents
Synthesis and biological evaluation of a new series of N-acyldiamines as potential antibacterial and antifungal agents
Ferreira, Bianca Da S.,De Almeida, Angelina M.,Nascimento, Thiago C.,De Castro, Pedro P.,Silva, Vania L.,Diniz, Claúdio G.,Le Hyaric, Mireille
supporting information, p. 4626 - 4629 (2015/01/08)
In continuation of our efforts to find new antimicrobial compounds, series of fatty N-acyldiamines were prepared from fatty methyl esters and 1,2-ethylenediamine, 1,3-propanediamine or 1,4-butanediamine. The synthesized compounds were screened for their antibacterial activity against Gram-positive bacteria (Staphylococcus aureus, Staphylococcus epidermidis), Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa) and for their antifungal activity against four species of Candida (C. albicans, C. tropicalis, C. glabrata and C. parapsilosis). Compounds 5a (N-(2-aminoethyl)dodecanamide), 5b (N-(2-aminoethyl)tetracanamide) and 6d (N-(3-aminopropyl)oleamide) were the most active against Gram-positive bacteria, with MIC values ranging from 1 to 16 μg/mL and were evaluated for their activity against 21 clinical isolates of methicillin-resistant S. aureus. All the compounds exhibited good to moderate antifungal activity. Compared to chloramphenicol, compound 6b displayed a similar activity (MIC50= 16 μg/mL). A positive correlation could be established between lipophilicity and biological activity.
