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[Antimycobacterial acting 2-hydroxyquinolizin-4-ones]
G Dannhardt1, T Kappe, W Meindl
1Institut für Pharmazeutische Chemie der Johann Wolfgang Goethe-Universität Frankfurt.
Archiv Der Pharmazie
|June 1, 1990
Abstract:
Reaction of ethyl 2-pyridyl acetates and activated malonates (magic malonates) leads to 1-ethoxycarbonyl-2-hydroxy-quinolizin-4-ones, which yield the corresponding C-1 unsubstituted derivatives by hydrolysis and decarboxylation. These compounds are catalytically hydrogenated to afford the corresponding tetrahydro derivatives. Significant inhibitory effects on mycobacterium tuberculosis H 37 Ra are shown, a structure-activity relationship is discussed.