3987-53-9Relevant academic research and scientific papers
Substance related with tophatib and preparation method and application thereof
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, (2019/01/08)
The invention discloses a substance related with tophatib and a preparation method and application thereof. The substance is named as N,N'-diacetyl{(3R,4R)-4-methyl-3-[methyl(7H-pyrrole[2,3-D]pyrimidine-4-yl)amine]piperidine-1-yl}imine. The impurity is characterized in that the generation level is lower in the condensation reaction process; however, the impurity has the uniform main functional groups with the tophatib, the cleaning effect is limited in the subsequent salting and refining process, and the influence to the qualities of crude drug and finished product of tophatib is larger; by detecting the existence of the impurity, the qualities of the raw material and preparation of the tophatib can be effectively determined.
Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, substrate-dependent modulators of insulin-degrading enzyme in amyloid-β hydrolysis
Charton, Julie,Gauriot, Marion,Guo, Qing,Hennuyer, Nathalie,Marechal, Xavier,Dumont, Julie,Hamdane, Malika,Pottiez, Virginie,Landry, Valerie,Sperandio, Olivier,Flipo, Marion,Buee, Luc,Staels, Bart,Leroux, Florence,Tang, Wei-Jen,Deprez, Benoit,Deprez-Poulain, Rebecca
, p. 184 - 193 (2014/05/06)
Insulin degrading enzyme (IDE) is a highly conserved zinc metalloprotease that is involved in the clearance of various physiologically peptides like amyloid-beta and insulin. This enzyme has been involved in the physiopathology of diabetes and Alzheimer's disease. We describe here a series of small molecules discovered by screening. Co-crystallization of the compounds with IDE revealed a binding both at the permanent exosite and at the discontinuous, conformational catalytic site. Preliminary structure-activity relationships are described. Selective inhibition of amyloid-beta degradation over insulin hydrolysis was possible. Neuroblastoma cells treated with the optimized compound display a dose-dependent increase in amyloid-beta levels.
Nickel(II) complexes with N-aralkyliminodiacetic acids: Preparation, spectroscopic, structural and thermal characterization
Smre?ki, Neven,Kukovec, Boris-Marko,Dakovi?, Marijana,Popovi?, Zora
, p. 122 - 129 (2013/07/25)
The reactions of N-aralkyl derivatives of iminodiacetic acid (H 2Bnida, H2Peida, H2Ppida, o-H2Cbida, Bn = benzyl, Pe = 2-phenylethyl, Pp = 3-phenylprop-1-yl, o-Cb = o-chlorobenzyl) with nickel(II) chloride hexahydrate or nickel(II) acetate tetrahydrate in aqueous solutions were studied. Five new nickel(II) complexes [Ni(Bnida)(H 2O)3]·H2O (1), [Ni(Peida)(H 2O)3] (2), [Ni(Ppida)(H2O)3] ·H2O (3a), [Ni(Ppida)(H2O)3] (3b) and [Ni(o-Cbida)(H2O)3] (4) were prepared and characterized by infrared spectroscopy and thermal analysis (TGA-DTA). The crystal structures of 1 and 3b were determined by single-crystal X-ray structural analysis. The octahedral coordination environment around the nickel(II) ion in 1 and 3b consists of an O,N,O′-tridentate N-aralkyliminodiacetate ion and three water molecules arranged in a fac-position. The molecules in the crystal structures of 1 and 3b are connected into a complicated hydrogen-bonded 2D network, dominated by the O-H?O hydrogen bonds. These 2D networks are in turn assembled into a 3D architecture only by weak van der Waals interactions.
RAPID DEBENZYLATION OF N-BENZYLAMINO DERIVATIVES TO AMINO-DERIVATIVES USING AMMONIUM FORMATE AS CATALYTIC HYDROGEN TRANSFER AGENT
Ram, Siya,Spicer, Leonard D.
, p. 515 - 516 (2007/10/02)
Various N-benzyl derivatives of amino acids and amines were deprotected to the corresponding free amino acids and amines using ammonium formate as the hydrogen source.
