[Antimycobacterial acting 2-hydroxyquinolizin-4-ones].
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.
Dannhardt
G
G
Institut für Pharmazeutische Chemie der Johann Wolfgang Goethe-Universität Frankfurt.
Kappe
T
T
Meindl
W
W
Schober
B
B
D055598:Chemical Phenomena; D002621:Chemistry; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D011807:Quinolizines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D011807:Quinolizines
Antimykobakteriell wirksame 2-Hydroxychinolizin-4-one.