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Synthetic Analogs of Phospholipid Metabolites as Antimalarials.
Final rept. 1 Jul 76-30 Sep 78,
LONG ISLAND JEWISH-HILLSIDE MEDICAL CENTER NEW HYDE PARK NY
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Analogs of phospholipids and their biosynthetic intermediates were synthetic targets as novel potential antimalarials. Targeted analogs contained one or more types of non-hydrolyzable groups, including ether, phosphonate, and phosphinate moieties. Synthetic routes varied with each target, and were quite complex for the cytidine-containing analogs of the biosynthetic intermediates, involving a number of novel steps. The phospholipid analogs were successfully prepared and submitted. However, during the course of the contract syntheses of the major cytidine-containing target compounds could not be completed, although a monophosphonate model analog was prepared and submitted. None of the thirteen compounds including three targets and one model target submitted displayed appreciable antimalarial activity in vivo in the standard test system. Author
APPROVED FOR PUBLIC RELEASE