Potential histidine decarboxylase inhibitors. 1. .alpha.- and .beta.-Substituted histidine analogs

Histidine analogues with alkyl substitution at Calpha and Cbeta were prepared as potential inhibitors of specific histidine decarboxylase. Activity was assessed in vitro using extracts of rat pyloric stomach and a radioisotopic assay of 14CO2 evolved from carboxyl-14C-labeled histidine. alpha-Substituted analogues (C2-C4) including 2-hydroxyethyl were less potent than alpha-methylhistidine; the alpha-n-butyl analogue was completely inactive at...