1.
Eur J Med Chem
; 160: 9-22, 2018 Dec 05.
Artigo
em Inglês
| MEDLINE
| ID: mdl-30316060
RESUMO
The design, synthesis and evaluation of a small series of potent amphiphilic norbornane antibacterial agents has been performed (compound 10 MICâ¯=â¯0.25⯵g/mL against MRSA). Molecular modelling indicates rapid aggregation of this class of antibacterial agent prior to membrane association and insertion. Two fluorescent analogues (compound 29 with 4-amino-naphthalimide and 34 with 4-nitrobenz-2-oxa-1,3-diazole fluorophores) with good activity (MICâ¯=â¯0.5⯵g/mL against MRSA) were also constructed and confocal microscopy studies indicate that the primary site of interaction for this family of compounds is the bacterial membrane.