57330-46-8Relevant academic research and scientific papers
INDOLE DERIVATIVES
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, (2009/10/22)
The present invention relates to indole derivatives which bind to the MCHl receptor. In separate aspects, the subject invention is directed to uses of said compounds in the preparation of a pharmaceutical composition for the treatment of obesity and CNS related disorders and to methods of treating said disorders comprising administering a therapeutically effective amount of a compound of the invention.
3-(2-(3-Pyridinyl)thiazolidin-4-oyl)indoles, a Novel Series of Platelet Activating Factor Antagonists
Sheppard, George S.,Pireh, Daisy,Carrera, George M.,Bures, Mark G.,Heyman, H. Robin,et al.
, p. 2011 - 2032 (2007/10/02)
(2RS,4R)-3-(2-(3-pyridinyl)thiazolidin-4-oyl)indoles represent a new class of potent, orally active antagonists of platelet activating factor (PAF). The compounds were prepared by acylation of the magnesium or zinc salts of substituted indoles with (2RS,4R)-2-(3-pyridinyl)-3-(tert-butoxycarbonyl)thiazolidin-4-oyl chloride. The 3-acylindole moiety functions as a hydrolytically stabilized and conformationally restricted anilide replacement, which imparts a considerable boost in potency to the series. Structure-activity relationships observed for substitution on the indole ring system are discussed. Members of the series compare favorably with other reported PAF antagonists.
3-arylcarbonyl and 3-cycloalkylcarbonyl-1-aminoalkyl-1H-indoles, compositions and use
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, (2008/06/13)
3-Arylcarbonyl- and 3-cycloalkylcarbonyl-1-aminoalkyl-1H-indoles, useful as analgesic, anti-rheumatic and anti-inflammatory agents, are prepared by reacting a 3-arylcarbonyl- or 3-cycloalkylcarbonylindole with an aminoalkyl halide in the presence of an acid-acceptor; by reacting a 1-aminoalkyl-1H-indole with an arylcarboxylic acid halide or a cycloalkanecarboxylic acid halide in the presence of a Lewis acid; or by reacting a 3-arylcarbonyl- or 3-cycloalkanecarbonyl-1-tosyloxyalky- or haloalkyl-1H-indole with an amine.
3-arylcarbonyl- and 3-cycloalkylcarbonyl-1-aminoalkyl-1H-indoles, compositions and use
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, (2008/06/13)
3-Arylcarbonyl- and 3-cycloalkylcarbonyl-1-aminoalkyl-1H-indoles, useful as analgesic, anti-rheumatic and anti-inflammatory agents, are prepared by reacting a 3-arylcarbonyl- or 3-cycloalkylcarbonylindole with an aminoalkyl halide in the presence of an acid-acceptor; by reacting a 1-aminoalkyl-1H-indole with an arylcarboxylic acid halide or a cycloalkanecarboxylic acid halide in the presence of a Lewis acid; or by reacting a 3-arylcarbonyl- or 3-cycloalkanecarbonyl-1-tosyloxyalky- or haloalkyl-1H-indole with an amine.
In pursuit of non narcotic analgetic and antiinflammatory agents. 1 carboxyalkyl 3 acylindoles
Allais,Meier,Mathieu,et al.
, p. 187 - 199 (2007/10/08)
The synthesis and study of different carboxyalcoyl 1 acyl 3 indoles has led to molecules endowed with analgesic properties associated with an anti inflammatory action of variable importance. In particular carboxymethyl 1 p chlorobenzoyl 3 methoxy 6 indole (RU 3959) has a strong analgesic activity and a remarkable tolerance which have been confirmed in clinical trials.
