Syntheses of new conformationally constrainedS‐[2‐[(1‐iminoethyl)amino] ethyl]homocysteine derivatives as potential nitric oxide synthase inhibitors

This is the authors' abstract. We don't add key points for this paper.

The efficient syntheses of two new types of conformationally constrained S‐[2‐[(1‐iminoethyl)amino]ethyl]homocysteine derivatives, 1‐amino‐3‐[2[(1‐iminoethyl)amino]ethylthio]cyclobutane carboxylic Acid (5) and (4S)‐4‐[[2‐[(1‐Iminoethyl)amino]ethyl]thio]‐L‐proline (6), are reported. These molecules represent the first attempts to probe conformational constraint near the α‐amino acid moiety of known homocysteine‐based inhibitors of nitric oxide synthase. Targets5and6were evaluated as potential inhibitors of the three human isoforms of nitric oxide synthase.