Accession Number:

ADA014991

Title:

Naphthyridine Antimalarial Agents

Descriptive Note:

Annual technical rept. 1 Apr 1974-31 Mar 1975

Corporate Author:

EXXON RESEARCH AND ENGINEERING CO LINDEN NJ GOVERNMENT RESEARCH LAB

Personal Author(s):

Report Date:

1975-04-01

Pagination or Media Count:

139.0

Abstract:

Interest in the 4-amino-1,5-naphthyridines as potential prophylactic antimalarial agents has been generated by the structural similarity of this ring system to both the 4- and 8-aminoquinolines. In our synthetic studies of this year, we sought to expand upon the derivatives of 4-amino-1,5-naphthyridine which are currently available in an effort to secure an optimal prophylactic antimalarial drug. Accordingly, as a result of our synthetic efforts, a total of sixty-one compounds comprising a variety of target structures, 1.5-naphthyridine intermediates and miscellaneous precursors have been prepared and submitted for biologic testing. While full biologic testing data are not yet available, results obtained for most of the target drugs submitted to WRAIR have disclosed no significant prophylactic activity in the lower dosage range 1.0 and 3.0 mg kg. However, one of the target structures, 2-hydroxy-4-5-isopropyl-aminopentylamino-1,5-naphthyridine, has now proven to be curative in the Rhesus monkey screen at a dosage level of 10.0 mgkg.

Subject Categories:

  • Pharmacology
  • Organic Chemistry

Distribution Statement:

APPROVED FOR PUBLIC RELEASE