Abstract：
:The design, synthesis and evaluation of a small series of potent amphiphilic norbornane antibacterial agents has been performed (compound 10 MIC = 0.25 μg/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 (MIC = 0.5 μg/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.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Hickey SM,Ashton TD,Boer G,Bader CA,Thomas M,Elliott AG,Schmuck C,Yu HY,Li J,Nation RL,Cooper MA,Plush SE,Brooks DA,Pfeffer FMdoi
10.1016/j.ejmech.2018.09.072subject
Has Abstractpub_date
2018-12-05 00:00:00pages
9-22eissn
0223-5234issn
1768-3254pii
S0223-5234(18)30858-4journal_volume
160pub_type
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