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):

Report Date:

1974-11-30

Pagination or Media Count:

45.0

Abstract:

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.

Subject Categories:

  • Pharmacology
  • Organic Chemistry

Distribution Statement:

APPROVED FOR PUBLIC RELEASE