Karel Waisser, Jiří Kuneš, Jiřina Stolaříková
Charles University, Prague, Czech Republic.
Ceska Slov Farm. 2012 Jun;61(3):127-9.
Derivatives of 3-phenyl-2H-1,3-benzoxazine-2,4(3H)-dione are active against Mycobacterium avium when substituted in position 7 with a methyl. One or two carbonyl groups have to be replaced with a thioxo group. High active derivatives are the compounds without substitution on the phenyl, or those substituted on the phenyl in position 3 or 4 with chlorine, bromine or a methyl. The substitution in position 3 and 4 with two atoms of chlorine lowers the activity. The compounds are active against INH resistant strains. We synthesized other 44 derivatives with a similar structure of the compounds as in the paper but substituted in position 7 with other substituents (chlorine, bromine methoxy). The activity against M. avium was poor. It can be concluded that a new group of compounds with an excellent activity against M. avium has been found.
3-苯基-2H-1,3-苯并恶嗪-2,4(3H)-二酮的衍生物在7位被甲基取代时对鸟分枝杆菌有活性。一个或两个羰基必须被硫代羰基取代。高活性衍生物是那些在苯基上无取代的化合物，或者是在苯基的3位或4位被氯、溴或甲基取代的化合物。在3位和4位被两个氯原子取代会降低活性。这些化合物对耐异烟肼菌株有活性。我们合成了其他44种与论文中化合物结构相似但在7位被其他取代基（氯、溴、甲氧基）取代的衍生物。它们对鸟分枝杆菌的活性较差。可以得出结论，已发现了一组对鸟分枝杆菌具有优异活性的新化合物。
