8-N-SUBSTITUTED-2H-ISOTHIAZOLO[5,4-B]QUINOLIZINE-3,4-DIONES AND RELATED COMPOUNDS AS ANTIINFECTIVE AGENTS

摘要

The invention provides compounds and salts of Formula (I) and Formula (II): which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula (I) and Formula (II). The variables A<SUB>1</SUB>, A<SUB>8</SUB>, R<SUB>2</SUB>, R<SUB>3</SUB>, R<SUB>5</SUB>, R<SUB>6</SUB>, R<SUB>7</SUB>, and R<SUB>9</SUB> are defined herein. Certain compounds of Formula (I) and Formula (II) disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula (I) or Formula (II) and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula (I) or Formula (II) as the only active agent or may contain a combination of compounds of Formula (I) and/or Formula (II) and one or more other active agents. The invention also provides methods for treating microbial and protozoal infections in animals.