689772-86-9Relevant academic research and scientific papers
Dual acting norepinephrine reuptake inhibitors and 5-HT2A receptor antagonists: Identification, synthesis and activity of novel 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles
Heffernan, Gavin D.,Coghlan, Richard D.,Manas, Eric S.,McDevitt, Robert E.,Li, Yanfang,Mahaney, Paige E.,Robichaud, Albert J.,Huselton, Christine,Alfinito, Peter,Bray, Jenifer A.,Cosmi, Scott A.,Johnston, Grace H.,Kenney, Thomas,Koury, Elizabeth,Winneker, Richard C.,Deecher, Darlene C.,Trybulski, Eugene J.
experimental part, p. 7802 - 7815 (2010/03/24)
The discovery of a series of 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles, dual acting norepinephrine reuptake inhibitors (NRIs) and 5-HT2A receptor antagonists, is described. The synthesis and structure-activity relationship (SAR) of this novel
Substituent effects on the electrophilic activity of nitroarenes in reactions with carbanions
Blazej, Sylwia,Makosza, Mieczyslaw
supporting information; experimental part, p. 11113 - 11122 (2009/11/30)
The effect on electrophilic activity of substituents located para, ortho, and meta to the nitro group of nitrobenzenes was determined by using vicarious nucleophilic substitution of hydrogen (VNS) with the carbanion of chloromethyl phenyl sulfone (1) as the model process. Values for the relative activities of substituted nitroarenes are given relative to nitrobenzene, which was taken as the standard. This process was chosen as a model reaction because it meets key criteria, such as the wide range of substituents that can be present on the nitrobenzene ring, a low sensitivity to steric hindrance, and in particular the possibility of ensuring conditions in which the overall relative rates of reaction in competitive experiments are equal to the relative rates of nucleophilic addition. The values of relative rates of addition, which were taken to be a measure of electrophilic activity, were determined by competitive experiments in which pairs of nitroarenes competed for the VNS reaction with carbanion of 1. A comprehensive set of data for effects of substituents on the electrophilic activity of nitroarenes is presented for the first time.
SULFONYL SUBSTITUTED 1H-INDOLES AS LIGANDS FOR THE 5-HYDROXYTRYPTAMINE RECEPTORS
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Page/Page column 79, (2008/06/13)
The present invention is directed to compounds of Formula I: which are modulators of the 5-hydroxtryptamine-6 and 5-hydroxytryptamine-2A receptors and which are inhibitors of norepinephrine reuptake. The compounds of the invention, and pharmaceutical comp
Substituted-3-sulfonylindazole derivatives as 5-hydroxytryptamine-6 ligands
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Page/Page column 83, (2010/11/25)
The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
