Naphthyridine Antimalarial Agents
Annual technical rept. 1 Apr 1973-31 Mar 1974
EXXON RESEARCH AND ENGINEERING CO LINDEN NJ GOVERNMENT RESEARCH LAB
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In synthetic studies, the authors 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 synthetic efforts, a total of one-hundred and three compounds comprising nineteen 1,5-naphthyridine target derivatives, forty-one 1,5-naphthyridine intermediates, and forty-three miscellaneous precursors have been prepared and submitted for biologic testing. While full biologic testing data are not yet available, test results obtained on most of the target drugs submitted have disclosed no significant prophylactic activity in the lower dosage range 1 mgkg. However, one of the target drugs, 2-hydroxy-4-5-isopropyl-amino pentylamino-1,5-naphthyridine, continues to afford protection after seventy days at a dosage level of 10 mgkg.
- Organic Chemistry