Conformationally restricted arginine analogues as inhibitors of human nitric oxide synthase

BG Shearer, S Lee, KW Franzmann, HAR White…

Index: 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. Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 13 p. 1763 - 1768

Full Text: HTML

Citation Number: 26

Abstract

Conformationally restricted analogues of the endogenous NOS substrate l-arginine and the arginine based NOS inhibitors NG-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 ...