186545-84-6Relevant academic research and scientific papers
Novel 3,4-Dihydroquinolin-2(1H)-one inhibitors of human glycogen phosphorylase a
Rosauer, Keith G.,Ogawa, Anthony K.,Willoughby, Chris A.,Ellsworth, Kenneth P.,Geissler, Wayne M.,Myers, Robert W.,Deng, Qiaolin,Chapman, Kevin T.,Harris, Georgianna,Moller, David E.
, p. 4385 - 4388 (2007/10/03)
The preparation of a series of substituted indoles coupled to six- and seven-membered cyclic lactams is described and their role as human glycogen phosphorylase a inhibitors discussed. The SAR of the indole moiety and lactam ring are presented.
Conformationally restricted arginine analogues as inhibitors of human nitric oxide synthase
Shearer, Barry G.,Lee, Shuliang,Franzmann, Karl W.,White, Helen A.R.,Sanders, Daniella C.J.,Kiff, Rachel J.,Garvey, Edward P.,Furfine, Eric S.
, p. 1763 - 1768 (2007/10/03)
Conformationally restricted analogues of the endogenous NOS substrate L- arginine and the arginine based NOS inhibitors N(G)-methyl-L-arginine (L- NMA) and Nδ-iminoethyl-L-ornithine (L-NIO) were synthesized for evaluation as inhibitors of human NOS. Incorporation of a phenyl ring into the C4-C5 backbone chain provided 2-aminophenylalanine analogues which retained potent NOS inhibition. Structurally related analogues of 3-aminophenylalanine were significantly weaker inhibitors.
