Conformationally restricted arginine analogues as inhibitors of human nitric oxide synthase

Article abstract of DOI:10.1016/S0960-894X(97)00309-0

Conformationally restricted analogues of the endogenous NOS substrate L- arginine and the arginine based NOS inhibitors N(G)-methyl-L-arginine (L- NMA) and Nδ-iminoethyl-L-ornithine (L-NIO) were synthesized for evaluation as inhibitors of human NOS. Incorporation of a phenyl ring into the C4-C5 backbone chain provided 2-aminophenylalanine analogues which retained potent NOS inhibition. Structurally related analogues of 3-aminophenylalanine were significantly weaker inhibitors.