Abstract
The asymmetric synthesis of an unprotected α-amino boronic acid analog of L-arginine 1a (boroarg-OH. 2 HCl) and its N α-acetyl derivative 1b (Ac-boroarg-OH. HCl) is described. These compounds were evaluated as substrates and inhibitors of recombinant nitric oxide synthases (NOS). Boroarg-OH 1a selectively inhibited inducible NOS (IC 50 = 50 μM) compared to the neuronal isoform (IC 50 = 300 μM).
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