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Synthesis of analogs of (1,4)-3- and 5-imino oxazepane, thiazepane, and diazepane as inhibitors of nitric oxide synthases.

Bioorganic & medicinal chemistry letters 2004 Dec 6; 14(23):5907-11

Link to PubMed abstract

Shankaran K K, Donnelly K KL, Shah S SK, Caldwell C CG, Chen P P, Hagmann W WK, Maccoss M M, Humes J JL, Pacholok S SG, Kelly T TM, Grant S SK, Wong K KK

Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. kothandaraman_shankaran@merck.com

A series of 3- and 5-imino analogs from oxazepane, thiazepane, and diazepane was prepared and evaluated as inhibitors of human nitric oxide synthesis (NOS). The most potent iNOS inhibitor was the thiazepane analog 25 (IC(50) = 0.19 microM).