THE INHIBITORY ACTION OF NAPHTHOQUINONES ON RESPIRATORY PROCESSES

Abstract

The first observation that certain 2-hydroxy-3-alkylnaphthoquinones exert an inhibitory action on respiratory processes was made by Wendel Wendel found that the relative effectiveness of these compounds in inhibiting the respiration of malarial parasites in vitro paralleled their ability to suppress malaria in animals. Our interest in these observations was aroused through our wartime collaboration with Dr. L. F. Fieser and his group, who were engaged in the synthesis and st,udy of these naphthoquinones as potential antimalarial drugs. The discovery of Wendel suggested that these naphthoquinones might be general respiratory poisons and that a simple oxidative enzyme system might be found which was inhibited by them. If this were so, it was reasoned that such an enzyme system might be employed to determine the relative potency of new naphthoquinone derivatives, and thus serve as a relatively simple screening test for the prompt guidance of the organic chemist synthesizing these compounds.