59576-23-7Relevant 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.
Arylalkyl-amines and -amides having anticonvulsant and neuroprotective properties
-
, (2008/06/13)
There is provided a method of treatment of neurological disorders, such as epilepsy, stroke and cerebral ischaemia, which comprises the administration of a compound of Formula I: STR1 wherein, Ar1 and Ar2, which may be the same or different, independently represent phenyl or phenyl substituted by one or more of amino, nitro, halogen, hydroxy, C1 to 6 alkoxy, C1 to 6 alkyl or cyano; R1 represents hydrogen, C1 to 6 alkyl, C1 to 6 alkoxycarbonyl; R2 represents hydrogen or COCH2 NH2 ; R3 represents hydrogen or C1 to 6 alkyl; in addition, when R2 represents hydrogen either one or both of Ar1 and Ar2 may also represent 2-, 3- or 4-pyridinyl and R1 may also represent trihalomethyl; or a pharmaceutically acceptable salt thereof. Some of the compounds of formula I are novel, and these are also provided, together with pharmaceutical compositions containing the novel compounds.
1-Phenylisoquinoline derivatives, pharmaceutical products containing these compounds and their use
-
, (2008/06/13)
1-Phenylisoquinoline derivatives of the general formula I STR1 and a process for their preparation are described. They act on the central nervous system, in particular as antidepressants.
