Selective heterocyclic amidine inhibitors of human inducible nitric oxide synthase
The potency and selectivity of a series of 5-hetero-2-iminohexahydroazepines were examined as inhibitors of the three human NOS isoforms. The effect of ring substitution of the 5-carbon for a heteroatom is presented. Potencies (IC50's) for these inhibitors are in the low micromolar range for hi-NOS with some examples exhibiting a 500× selectivity versus hec-NOS.
Moormann, Alan E.,Metz, Sue,Toth, Mihaly V.,Moore, William M.,Jerome, Gina,Kornmeier, Christine,Manning, Pamela,Hansen Jr., Donald W.,Pitzele, Barnett S.,Webber
p. 2651 - 2653
(2007/10/03)
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