Synthesis of some novel 2-oxo-pyrano(2,3-b)- and 2-oxo-pyrido(2,3-b)quinoline derivatives as potential antimalarial, diuretic, clastogenic and antimicrobial agents.
The 2-chloro-3-formyl quinoline derivatives (1a-e) on treatment with acetic anhydride and sodium acetate, afforded the corresponding novel 2-oxopyrano(2,3-b) quinoline derivatives (2a-e), and these were subjected to ammonia treatment to yield the corresponding naphthyridine derivatives (3a-e). The prepared compounds (2a-e) were tested for their antimalarial, diuretic, clastogenic and antimicrobial properties. Not all the compounds showed a diuretic effect and the significant increase in the frequency of micronuclei shows that they are non-clastogens, whereas the 7-chloro derivative (2e) was a very effective antimalarial agent against the mosquito species. All the compounds were found to have optimum antimicrobial activity against Staphylococcus aureus, Escherichia coli and Salmonella typhi. Compounds 2d and 2e were found to be most active against the bacteria tested.
Sekar
M
M
Department of Chemistry, Bharathiar University, Coimbatore, India.
Prasad
K J
KJ
D000818:Animals; D000852:Anopheles / Q000187:drug effects*; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis*; D000962:Antimalarials / Q000138:chemical synthesis*; D001854:Bone Marrow Cells / Q000187:drug effects; D004232:Diuretics / Q000138:chemical synthesis*; D004926:Escherichia coli / Q000187:drug effects; D007814:Larva / Q000187:drug effects; D051379:Mice; D008826:Microbial Sensitivity Tests; D009153:Mutagens / Q000737:chemistry; D015363:Quinolones / Q000138:chemical synthesis*; D012485:Salmonella typhi / Q000187:drug effects; D013211:Staphylococcus aureus / Q000187:drug effects
D000900:Anti-Bacterial Agents; D000962:Antimalarials; D004232:Diuretics; D009153:Mutagens; D015363:Quinolones