4836-98-0Relevant academic research and scientific papers
Discovery and structural analyses of S-adenosyl-l-homocysteine hydrolase inhibitors based on non-adenosine analogs
Nakao, Akira,Suzuki, Hiroko,Ueno, Hiroaki,Iwasaki, Hiroshi,Setsuta, Tomofumi,Kashima, Akiko,Sunada, Shinji
, p. 4952 - 4969 (2015/08/03)
Optimization of a new series of S-adenosyl-l-homocysteine hydrolase (AdoHcyase) inhibitors based on non-adenosine analogs led to very potent compounds 14n, 18a, and 18b with IC50 values of 13 ± 3, 5.0 ± 2.0, and 8.5 ± 3.1 nM, respectively. An X-ray crystal structure of AdoHcyase with NAD+ and 18a showed a novel open form co-crystal structure. 18a in the co-crystals formed intramolecular eight membered ring hydrogen bond formations. A single crystal X-ray structure of 14n also showed an intramolecular eight-membered ring hydrogen bond interaction.
Carbazates as potent inhibitors of hormone-sensitive lipase
De Jong, Johannes C.,Sorensen, Lotte G.,Tornqvist, Hans,Jacobsen, Poul
, p. 1741 - 1744 (2007/10/03)
The central role of adipose tissue hormone-sensitive lipase in regulating fatty acid metabolism makes it a potential pharmacological target for the prevention of peripheral insulin resistance in obese, prediabetic and diabetic individuals. The synthesis of a new series of carbazates is presented. Modification of the phenolic 4-position in a series of 1,2,3,4- tetrahydroisoquinoline and morpholine derived carbazates, yielded inhibitors of the catalytic activity of this enzyme with nanomolar potency.
Diuretic agents related to indapamide: III - Synthesis and pharmacological activity of N-(4-chloro-3-sulfamoylbenzamido)-1,2,3,4-tetrahydroquinolines 1,2,3,4-tetrahydroisoquinolines.
Landriani,Barlocco,Pinna,Demontis,Miele,Enrico,Anania
, p. 1059 - 1068 (2007/10/02)
A series of N-(4-chloro-3-sulfamoylbenzamido)-1,2,3,4-tetrahydroquinoline (IV-1) and isoquinoline (IV-2) have been synthesized and their diuretic and antihypertensive activities evaluated. While none of the test compounds was found to be provided with ant
METAL-ASSISTED REACTIONS-PART 11 RAPID REDUCTION OF N-NITROSOAMINES TO N,N-DISUBSTITUTED HYDRAZINES; THE UTILITY OF SOME LOW-VALENT TITANIUM REAGENTS
Entwistle, Ian D.,Johnstone, A. W.,Wilby, Anna H.
, p. 419 - 423 (2007/10/02)
The rapid reduction of N-nitrosoamines to N,N-disubstituted hydrazines by a low-valent titanium reagent is described.The reagent is selective in that many other functional groups are unaffected by it.The nature of the low-valent titanium reagent is discussed in terms of experimental results of comparisons of its reactivity and that of other low-valent titanium reducing agents.
