Accession Number : ADA007248


Title :   Synthesis of Some 4-Quinolones and Related Structures for Evaluation as Potential Antimalarial Agents


Descriptive Note : Annual rept. no. 2 (Final), 1 May 73-30 Nov 74,


Corporate Author : BRIDGEPORT UNIV CT DEPT OF CHEMISTRY


Personal Author(s) : Casey, Adria C.


Full Text : http://www.dtic.mil/get-tr-doc/pdf?AD=ADA007248


Report Date : 30 NOV 1974


Pagination or Media Count : 45


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.


Descriptors :   *ANTIMALARIALS , *QUINOLINES , TOXICITY , SYNTHESIS(CHEMISTRY) , BIOASSAY , LABORATORY ANIMALS , CHEMOTHERAPEUTIC AGENTS , PLASMODIUM , KETONES , MALARIA , PHARMACOLOGY , PYRIDINES


Subject Categories : PHARMACOLOGY
      ORGANIC CHEMISTRY


Distribution Statement : APPROVED FOR PUBLIC RELEASE