56541-16-3Relevant academic research and scientific papers
GLYCOSIDASE INHIBITORS
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Page/Page column 76, (2014/10/15)
Compounds of formula (I) wherein X1, X2, W, R1 to R5, L and m have the meaning according to the claims, are glucosidase inhibitors, and can be employed, inter alia, for the treatment of Alzheimer's disease.
NOVEL COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS FOR USE IN TREATING METABOLIC DISORDERS
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Page/Page column 49, (2011/12/14)
The present invention is directed to novel compounds of formula (I) and their use in treating metabolic diseases.
NG-Allyl- and NG-Cyclopropyl-L-arginine: Two Novel Inhibitors of Macrophage Nitric Oxide Synthase
Olken, Norman M.,Marletta, Michael A.
, p. 1137 - 1144 (2007/10/02)
NG-Methyl-L-arginine has recently been shown to inactivate the inducible murine macrophage nitric oxide (.NO) synthase (Olken, N.M.; Rusche, K.M.; Richards, M.K.; Marletta, M.A.Biochem.Biophys.Res.Commun. 1991, 177, 828-833).NG-Allyl-L-arginine and NG-cyclopropyl-L-arginine were synthesized as potential mechanism-based enzyme inhibitors to exploit the chemistry presumed to occur at the active site.NG-Cyclopropyl-L-arginine was found to be a potent reversible inhibitor with a Ki = 7.7 μM.NG-Allyl-L-arginine was found to be both a potent reversible (Ki = 2.1 μM) and irreversible inhibitor of the enzyme.The irreversible inhibition demonstrated pseudo-first-order inactivation kinetics with kinact = 0.026 min-1 and Ki = 3.4 μM.Stereospecific protection of the inactivation was afforded by L-arginine, and saturability of the inactivation rate was observed.Our studies indicate that both reversible and irreversible inhibition of the inducible .NO synthase can be achieved with relatively simple modifications of the substrate L-arginine.
