85328-30-9Relevant academic research and scientific papers
METHOD OF INHIBITING APOLIPOPROTEIN-E EXPRESSION COMPRISING ADMINISTERING A TRIARYLMETHYL AMINE COMPOUND
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, (2014/02/15)
This invention offers an effective method of inhibiting the expression of apolipoprotein E by mammalian cells. Apolipoprotein E is a protein that plays a significant role in the development of Alzheimer's Disease in humans. The method comprises administering an effective amount of a triarylmethyl amine compound having the general formula: wherein the R1 group may comprise acyclic amines and aliphatic amines. The R2 group may comprise one of three aryl varieties: aryl, substituted aryl, or heterocycle. Triarylamine compounds inhibit apolipoprotein E expression in mammalian cells. In one aspect of the invention the mammalian cells may be human cells, and more specifically may be human brain cells.
Design, synthesis and identification of a new class of triarylmethyl amine compounds as inhibitors of apolipoprotein e production
Singh, Mandeep,Schott, Jason T.,Leon, Martin A.,Granata, Robert T.,Dhah, Harkiran K.,Welles, Jason A.,Boyce, Michelle A.,Oseni-Olalemi, Hafeez S.,Mordaunt, Charles E.,Vargas, Anthony J.,Patel, Nilay V.,Maitra, Santanu
, p. 6252 - 6255 (2012/10/29)
We have identified a new class of triarylmethyl amine compounds that can inhibit apolipoprotein E (apoE) production. ApoE is a cholesterol- and lipid-carrier protein implicated in aging, atherosclerosis, Alzheimer's Disease (AD), and other neurological and lipid-related disorders. Attenuation of apoE production is generally considered to be of therapeutic value. A majority of the apoE in the brain is produced by astrocytes. Here, we describe the design, synthesis, and biological screening of a small library of compounds that led to the identification of four triarylmethyl amines as potent inhibitors of apoE production in CCF-STTG1 astrocytoma cells.
Influence of some novel N-substituted azoles and pyridines on rat hepatic CYP3A activity
Slama, James T.,Hancock, Julie L.,Rho, Taikyun,Sambucetti, Lidia,Bachmann, Kenneth A.
, p. 1881 - 1892 (2008/04/18)
A series of N-substituted heteroaromatic compounds structurally related to clotrimazole was synthesized, and the effects of these compounds on ethosuximide clearance in rats were determined as a measure of their abilities to induce cytochrome P4503A (CYP3A) activity. Ethosuximide clearance and in vitro erythromycin N-demethylase activity were shown to correlate. In this series, imidazole or other related heteroaromatic 'head groups' were linked to triphenylmethane or other phenylmethane derivatives. Within the series, it was found that 1-triphenylmethane-substituted imidazoles elicited the greatest increase in CYP3A activity, and that among the triphenylmethyl-substituted imidazoles, the highest activities were achieved by the substitution of F- or Cl- in either the meta or para position of one of the phenyl rings. Diphenylmethylsubstituted pyridine was effectively devoid of activity. Compounds eliciting the largest increase in CYP3A activity (viz. 1-[(3-fluorophenyl)diphenylmethyl]imidazole, 1-[(4- fluorophenyl)diphenylmethyl]imidazole, and 1-[tri-(4- fluorophenyl)methyl]imidazole) produced little or no increase in ethoxyresorufin O-dealkylase (EROD) activity (i.e. CYP1A), whereas benzylimidazole, which elicited only a small increase in CYP3A activity, produced an almost 9-fold increase in CYP1A activity. For a series of eleven compounds exhibiting a wide range of influence on CYP3A activity, a positive correlation was found between ethosuximide clearance and hepatic CYP3A mRNA levels.
Methacrylic ester useful as an optical resolving agent
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, (2008/06/13)
A methacrylic ester which functions as the main unit of a polymer or copolymer which is useful as an agent to optically resolve racemic mixtures of compounds.
