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ID: ALA1133982

Journal: Bioorg Med Chem Lett

Title: Selective heterocyclic amidine inhibitors of human inducible nitric oxide synthase.

Authors: Moormann AE, Metz S, Toth MV, Moore WM, Jerome G, Kornmeier C, Manning P, Hansen DW, Pitzele BS, Webber RK.

Abstract: 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 (IC(50)'s) for these inhibitors are in the low micromolar range for hi-NOS with some examples exhibiting a 500x selectivity versus hec-NOS.

CiteXplore: 11551770

DOI: 10.1016/s0960-894x(01)00523-6