Synthesis of Some 4-Quinolones and Related Structures for Evaluation as Potential Antimalarial Agents
Annual rept. no. 2 (Final), 1 May 73-30 Nov 74,
BRIDGEPORT UNIV CT DEPT OF CHEMISTRY
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The object was to synthesize and submit for antimalarial evaluation new compounds related to either endochin 2-methyl-3-heptyl-7-methoxy-41H- quinolone or the 3-carbomethoxy-41H-quinolones that had shown moderate to good antimalarial activity. A total of 31 new compounds, 16 of these target compounds, were synthesized and submitted for antimalarial evaluation. Compound BD26235 N-hydroxy-4-oxo-2-methyl-3-n-heptyl-7-methoxyquinolone, endochin-N- oxide, when tested against sporozoite-induced P. gallinaceum infection in chicks, cured 2 out of 5 chicks at a dose of 30 mgKg 3 out of 5 chicks at a dose of 120 mgKg and 5 out of 5 chicks at a dose of 480 mgKg with no toxicity at any dose level. Compound BE11382 3-carboethoxy-6-n-butyl-7- phenoxyethylmercapto-41Hquinolone was found to increase the mean survival time of the treated animals over that of the control group by 3.5 days at a dose of 320 mgKg and by 5.3 days at a dose of 640 mgKg with no toxicity when tested in the blood-induced P. berghei mouse test.
- Organic Chemistry