DNA binding ligands with in vivo efficacy in murine models of bacterial infection: optimization of internal aromatic amino acids.
Bürli RW, Kaizerman JA, Duan JX, Jones P, Johnson KW, Iwamoto M, Truong K, Hu W, Stanton T, Chen A, Touami S, Gross M, Jiang V, Ge Y, Moser HE.
DNA binding ligands with potent antimicrobial activity against Gram-positive bacteria were further optimized by variation of the internal aromatic amino acids. This modification led to compounds with improved in vivo efficacy in lethal murine models of peritonitis (methicillin-resistant S. aureus, MRSA) and lung infection (S. pneumoniae).