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

作者信息

Shankaran K, Donnelly Karla L, Shah Shrenik K, Caldwell Charles G, Chen Ping, Hagmann William K, Maccoss Malcolm, Humes John L, Pacholok Stephen G, Kelly Theresa M, Grant Stephan K, Wong Kenny K

机构信息

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

出版信息

Bioorg Med Chem Lett. 2004 Dec 6;14(23):5907-11. doi: 10.1016/j.bmcl.2004.09.019.

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).