43071-00-7Relevant academic research and scientific papers
Substituted (1,2-Diarylethyl)amide Acyl-CoA:Cholesterol Acyltransferase Inhibitors: Effect of Polar Groups on in Vitro and in Vivo Activity
Clader, John W.,Berger, Joel G.,Burrier, Robert E.,Davis, Harry R.,Domalski, Martin,et al.
, p. 1600 - 1607 (2007/10/02)
Substituted (1,2-diarylethyl)amides have been prepared and evaluated for their ability to inhibit microsomal acyl-CoA:cholesterol acyltransferase activity in vitro and to lower hepatic cholesteryl ester content in vivo in a cholesterol-fed hamster.Simple unsubstituted (diarylethyl)amides were potent inhibitors in vitro but showed poor activity in vivo.Introduction of polar groups at specific locations on the diarylethylamine moiety decreased in vitro activity but increased in vivo activity.Both effects were highly structure dependent, suggesting specific interactions which were mediating activity in each model.Optimization of these opposing effects led to compounds which were potent in both models.
Regiochemistry on Photoamination of Stilbene Derivatives with Ammonia via Electron Transfer
Yasuda, Masahide,Isami, Toshihiro,Kubo, Jun-ichi,Mizutani, Manabu,Yamashita, Toshiaki,et al.
, p. 1351 - 1354 (2007/10/02)
The regiochemistry of photoamination of 1,2-diarylethene (1) with ammonia in the presence of p-dicyanobenzene (DCNB) has been investigated.The photoamination of stilbene and p,p'-dimethoxystilbene gave 1-amino-1,2-diphenylethane and 1-amino-1,2-bis(p-methoxyphenyl)ethane, respectively.The photoamination of unsymmetric 1-aryl-2-phenylethene having an alkoxy group on the para position occurred selectively to give 1-amino-2-aryl-1-phenylethane.On the other hand, the photoamination of 1-aryl-2-phenylethene having a methyl and chloro group on the para position or methoxy group on the meta and ortho positions gave both 1-amino-2-aryl-1-phenylethane and 1-amino-1-aryl-2-phenylethane.The regiochemistry is related with the distribution of positive charge in the cation radicals of 1 generated from photochemical electron transfer to DCNB.
N-acyl-tetrahydroisoquinolines as inhibitors of acyl-coenzyme a:cholesterol acyl transferase
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, (2008/06/13)
N-acyltetrahydroisoquinolines including novel compounds of the formula STR1 wherein R1 is a C10-C25 alkyl chain; a substituted C10-C25 alkyl chain; an interrupted C10-C25 alkyl chain; a substituted interrupted C10-C25 alkyl chain; diphenylamino
α-phenyl-β-(3,4-dimethoxy)phenethylamines: Novel inhibitors of choline acetyltransferase from Torpedo electric organ
Shafik,Soliman,El-Hawash,Morshedy,Mansour
, p. 1548 - 1550 (2007/10/02)
Some derivatives of α-phenyl-β-(3,4-dimethoxy)phenethylamine that might bear a certain conformational resemblance to choline were prepared. The in vitro inhibition of choline acetyltransferase from Torpedo electric organ was investigated. These compounds
