1.
Bioorg Med Chem Lett
; 19(18): 5359-62, 2009 Sep 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-19682900
RESUMO
In the search for new antibacterial agents, the enzyme FabI has been identified as an attractive target. Employing a structure guided approach, the previously reported ene-amide series of FabI inhibitors were expanded to include 2,3,4,5-tetrahydro-1H-pyrido[2,3-b and e][1,4]diazepines. These novel series incorporate additional H-bonding functions and can be more water soluble than their naphthyridinone progenitors; diazepine 16c is shown to be efficacious in a mouse infection model.