A Study of a-Chloroketonic Inhibitors of Corticosteroid Acetyltransferase
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Various a-chloro-acetophenones and a-chloro methyl ketones were tested for inhibition of the enzyme corticosteroid acetyl transferase in hopes of finding a very effective inhibitor of the enzyme. This inhibitor could then possibly be used to purify the enzyme and/or after further study an analog for the corticosteroids themselves. The research showed various properties necessary for effective inhibition. There is a critical distance necessary between the a-chloro ketone function and the ring. The substituents on the ring structure of the inhibitor have to be activating as there is a definite positive electronic effect between the ring and the enzyme. The inhibitor should also show some configurational constraint. The most effective inhlhitor-TPCK-is now being used in further research.