Synthesis of analogs of (1,4)-3- and 5-imino oxaze...[Bioorg Med Chem Lett. 2004]

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1: Bioorg Med Chem Lett. 2004 Dec 6;14(23):5907-11. Links

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

Shankaran K, Donnelly KL, Shah SK, Caldwell CG, Chen P, Hagmann WK, Maccoss M, Humes JL, Pacholok SG, Kelly TM, Grant SK, Wong 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).

PMID: 15501067 [PubMed - indexed for MEDLINE]

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

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