The potency and selectivity of a series of 5-hetero-2-iminohexahydroazepine
s were examined as inhibitors or the three human NOS isoforms. The effect o
r ring substitution of the 5-carbon for a heteroatom is presented. Potencie
s (IC50's) for these inhibitors are in the low micromolar range for hi-NOS
with some examples exhibiting a 500x selectivity versus hec-NOS. (C) 2001 E
lsevier Science Ltd. All rights reserved.