| abstract |
Benzo[de]isoquinoline-1,3-dione of Formulaor a pharmaceutically acceptable salt thereof wherein R is hydrogen or a protecting group typically used in the art for protecting alcohols and R1-R5 are each independently chosen from H, Cl, Br, F, straight or branched alkyl C1-C8 alkyl, C3-C8 cycloalkyl, heterocycle or bridged heterocycle of 4-9 atoms containing 1-3 heteroatoms, -(CR'2)nOR6, -(CR'2)nN(R6)2, -(CR'2)nNR6COR7, -(CR'2)nNR6SO2OR7, -(CR'2)nNR6SO2 N(R6)2, -(CR'2)nOSO2 N(R6)2, -(CR'2)nCN, -(CR'2)n(NOR6)R7, NO2, CF3, -(CR'2)nSOmR7, -(CR'2)nSOmR7, -(CR'2)nCO2R6, -(CR'2)nCON(R6)2, Ph, and any two of R1-R5 may form a substituted or unsubstituted ring of 5-7 total atoms having 0-2 heteroatoms are claimed which are selective inhibitors of bacterial DNA gyrase and DNA topoisomerase useful in antibacterial agents. Methods for their preparation and formulation as well as novel intermediates useful in the preparation of the final products are also claimed. |