Bioorganic and Medicinal Chemistry Letters p. 1763 - 1768 (1997)
Update date:2022-07-30
Topics:
Shearer, Barry G.
Lee, Shuliang
Franzmann, Karl W.
White, Helen A.R.
Sanders, Daniella C.J.
Kiff, Rachel J.
Garvey, Edward P.
Furfine, Eric S.
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.
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