Relationship between structure and antibacterial activity of lipophilic N-acyldiamines.

We report in this work the preparation and antibacterial evaluation of a series of N-monoacylated diamines against six Gram-positive and 11 Gram-negative bacteria. The results obtained showed the existence of relationship between lipophilicity and antibacterial activity of the tested compounds. The best results were obtained against Gram-positive bacteria for compounds having a 10-12 carbons alkyl chain. Compound 4e was the most active against Microccus lentus (MIC=2 microg/mL), Staphylococcus aureus ATCC 29213 (MIC=4 microg/mL) and Enterobacter aerogenes CDC 1680 (MIC=8 microg/mL). (c) 2009 Elsevier Masson SAS. All rights reserved.