Collect. Czech. Chem. Commun. 1993, 58, 2977-2982

New Groups of Potential Antituberculotics: 3-Aryl-2H,4H-benz[e][1,3]oxazine-2,4-diones. Comparison of the Topliss Approach with Regression Analysis

Karel Waissera, Lenka Kubicováa, Věra Klimešováa and Želmíra Odlerováb

a Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, 501 65 Hradec Králové, Czech Republic
b Institute of Preventive and Clinical Medicine, 833 01 Bratislava, Slovak Republic


3-Phenyl-2H,4H-benz[e][1,3]oxazine-2,4-dione (I) and its derivatives II - XI, substituted on the phenyl ring, can be regarded as a new group of potential antituberculotics. Their activity increases with increasing electron-accepting properties of the substituents. introduction of bromine into the position 6 also positively influences the activity. the compounds are active in vitro against Mycobacterium tuberculosis and M. kansasii. The activity of some of them (VIII, IX0 exceeds that of commercial tuberculostatics used as standards.