Bioorganic and Medicinal Chemistry Letters p. 2651 - 2653 (2001)
Update date:2022-08-11
Topics:
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
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.
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