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Bioorg Med Chem Lett. 2001 Oct 8;11(19):2651-3.

Selective heterocyclic amidine inhibitors of human inducible nitric oxide synthase.

Author information

1
Pharmacia, 700 Chesterfield Parkway North, St. Louis, MO 63198, USA. alan.e.moormann@pharmacia.com

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.

PMID:
11551770
DOI:
10.1016/s0960-894x(01)00523-6
[Indexed for MEDLINE]

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