55047-81-9Relevant academic research and scientific papers
Novel synthesis of sterically hindered N-substituted lactams from imides
Sannigrahi, Mousumi,Pinto, Patrick,Chan,Shih, Neng-Yang,George Njoroge
, p. 4877 - 4880 (2006)
An efficient and practical synthesis of sterically hindered N-substituted lactams has been developed starting from simple starting materials. The stereochemistry of the synthetically useful N,N acetal intermediate has been established.
Amidino derivatives useful as nitric oxide synthase inhibitors
-
, (2008/06/13)
The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.
Amidino dervatives useful as nitric oxide synthase inhibitors
-
, (2008/06/13)
The current invention discloses useful pharmaceutical compositions containing azepine derivatives useful as nitric oxide synthase inhibitors.
Substituted 2-iminopiperidines as inhibitors of human nitric oxide synthase isoforms
Webber, R. Keith,Metz, Suzanne,Moore, William M.,Connor, Jane R.,Currie, Mark G.,Fok, Kam F.,Hagen, Timothy J.,Hansen Jr., Donald W.,Jerome, Gina M.,Manning, Pamela T.,Pitzele, Barnett S.,Toth, Mihaly V.,Trivedi, Mahima,Zupec, Mark E.,Siong Tjoeng
, p. 96 - 101 (2007/10/03)
A series of analogues of 2-iminopiperidine have been prepared and shown to be potent inhibitors of the human nitric oxide synthase (NOS) isoforms. Methyl substitutions on the 4-position (3) or 4- and 6-positions (8) afforded the most potent analogues. These compounds exhibited IC50 values of 0.1 and 0.08 μM, respectively, for hiNOS inhibition. Substitution with cyclohexylmethyl at the 6-position (13) afforded an inhibitor that showed the best selectivity for hiNOS versus heNOS (heNOS IC50/hiNOS IC50 = 64). Following oral administration, inhibitors were found to decrease serum nitrite/nitrate levels in an in vivo rat endotoxin assay. This series of 2- iminopiperidines were prepared via the described synthetic methodologies. The effect of ring substitutions on potency and selectivity for this class of cyclic amidines as NOS inhibitors is described.
