90872-67-6Relevant 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.
THERAPEUTIC AGENT FOR CEREBRAL INFARCTION
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, (2012/08/08)
The invention provides a therapeutic drug for ischemic stroke. The therapeutic drug has the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof, as an active ingredient.
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.
