Synthesis of Some 4-Quinolones and Related Structures for Evaluation as Potential Antimalarial Agents
Abstract
The object was to synthesize and submit for antimalarial evaluation new compounds related to either endochin (2-methyl-3-heptyl-7-methoxy-4(1H)- quinolone) or the 3-carbomethoxy-4(1H)-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 mg/Kg; 3 out of 5 chicks at a dose of 120 mg/Kg and 5 out of 5 chicks at a dose of 480 mg/Kg with no toxicity at any dose level. Compound BE11382 (3-carboethoxy-6-n-butyl-7- phenoxyethylmercapto-4(1H)quinolone) 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 mg/Kg and by 5.3 days at a dose of 640 mg/Kg with no toxicity when tested in the blood-induced P. berghei mouse test.
Document Details
- Document Type
- Technical Report
- Publication Date
- Nov 30, 1974
- Accession Number
- ADA007248
Entities
People
- Adria C. Casey
Organizations
- University of Bridgeport