Bürli Roland W, Jones Peter, McMinn Dustin, Le Quan, Duan Jian-Xin, Kaizerman Jacob A, Difuntorum Stacey, Moser Heinz E
Genesoft Pharmaceuticals Inc., 7300 Shoreline Court, South San Francisco, CA 94080, USA.
Bioorg Med Chem Lett. 2004 Mar 8;14(5):1259-63. doi: 10.1016/j.bmcl.2003.12.043.
The synthesis and in vitro potency of DNA minor-groove binding antibacterials lacking the C-terminal amide bond are described. The crescent shaped molecules bear the positively charged amino group at an internal pyrrole unit instead of the C-terminus. Three structural parameters were investigated: the N-terminal unit, the internal amino group, and the C-terminal ring system. Several compounds demonstrated good in vitro potency against various Gram-positive bacteria and some molecules were moderately active against Escherichia coli, a representative Gram-negative strain.
