TY - JOUR
T1 - Synthesis of analogs of (1,4)-3- and 5-imino oxazepane, thiazepane, and diazepane as inhibitors of nitric oxide synthases
AU - Shankaran, K.
AU - Donnelly, Karla L.
AU - Shah, Shrenik K.
AU - Caldwell, Charles G.
AU - Chen, Ping
AU - Hagmann, William K.
AU - MacCoss, Malcolm
AU - Humes, John L.
AU - Pacholok, Stephen G.
AU - Kelly, Theresa M.
AU - Grant, Stephan K.
AU - Wong, Kenny K.
PY - 2004/12/6
Y1 - 2004/12/6
N2 - The preparation and SAR of a series of iNOS inhibitors leading to the most potent compound, incorporating a (1,4)-5-imino thiazepane (R = n-Pr) is disclosed. 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 μM).
AB - The preparation and SAR of a series of iNOS inhibitors leading to the most potent compound, incorporating a (1,4)-5-imino thiazepane (R = n-Pr) is disclosed. 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 μM).
KW - NOS synthase
UR - http://www.scopus.com/inward/record.url?scp=7044269371&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=7044269371&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2004.09.019
DO - 10.1016/j.bmcl.2004.09.019
M3 - Article
C2 - 15501067
AN - SCOPUS:7044269371
SN - 0960-894X
VL - 14
SP - 5907
EP - 5911
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 23
ER -