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).
de Almeida
Camila G
CG
Departamento de Química, Instituto de Ciências Exatas, Universidade Federal de Juiz de Fora, 36036-900 Juiz de Fora, MG, Brazil.
Garbois
Gabriela D
GD
Amaral
Lorena M
LM
Diniz
Cláudio C
CC
Le Hyaric
Mireille
M
D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D003959:Diamines / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D003959:Diamines