- Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 1: Identification and synthesis of phenyl-tetrazolyl acetophenones
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We have identified and synthesized a series of aryl-tetrazoyl acetophenones as positive allosteric potentiators of the metabotropic glutamate receptor 2. Structure activity relationship studies directed toward improving the potency and level of potentiation led to the discovery of 22 (EC50 = 93 nM, 128% potentiation). We have identified and synthesized a series of aryl-tetrazoyl acetophenones as positive allosteric potentiators of the metabotropic glutamate receptor 2. Structure activity relationship studies directed toward improving the potency and level of potentiation led to the discovery of 22 (EC50 = 93 nM, 128% potentiation).
- Pinkerton, Anthony B.,Cube, Rowena V.,Hutchinson, John H.,Rowe, Blake A.,Schaffhauser, Hervé,Zhao, Xiumin,Daggett, Lorrie P.,Vernier, Jean-Michel
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p. 5329 - 5332
(2007/10/03)
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- Synthesis of the leukotriene antagonist ablukast
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An efficient synthesis of the leukotriene antagonist ablukast (5) has been achieved starting from 2,4-dihydroxyacetophenone. The latter, on a Claisen condensation with ethyl oxalate, followed by hydrogenation, gave the chromane ester 7, which was subjected to a Fries rearrangement (AcOH/BF3·OEt2) and the product, after transesterification with methanol, was alkylated with 5-bromo-1-pentanyl acetate to afford the acetate 9. A novel methanolysis of 9 with methanol in the presence of tetra-n-butylammonium hydroxide followed by mesylation of the derived alcohol furnished the mesylate 10. Alkylation of the acetophenone derivative 16 with 10 using K2CO3 in the presence of tris(3,6-dioxaheptyl)amine and saponification gave 5.
- Manchand,Micheli,Saposnik
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p. 9391 - 9398
(2007/10/02)
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- STEREOSELECTIVE SYNTHESIS OF LEUKOTRIENE ANTAGONISTS
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The present invention relates to a stereo-selective synthesis of leukotriene antagonists. More particularly, this invention relates to the stereo-selective synthesis of (βS,γR) and (βR,γS)-4-((3-(4-acetyl-3-hydroxy-2-propyl(phenoxy)propyl)-thio-γ-hydroxy-
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- Process for leukotriene antagonists
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1,3-Dialkylbenzenes are acylated and deprotected in a mixture of acetic or propionic acid and hydrobromic acid. The dihydroxyphenones thus produced are intermediates in the synthesis of leukotriene antagonists.
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- Stereoselective synthesis of leukotriene antagonists
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The present invention relates to a stereo-selective synthesis of leukotriene antagonists. More particularly, this invention relates to the stereo-selective synthesis of (βS,γR) and (βR,γS)--4-((3-(4-acetyl-3-hydroxy-2-propyl(phenoxy)propyl)-thio)-γ-hydroxy-β-methylbenzenebutanoic acid, and related compounds. These compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders, inflammation and pain in mammals, especially humans. The compounds are also useful for inducing cytoprotection in mammals, especially humans.
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- Novel benzopyran derivatives
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7-[3-(4-Acetyl-3-hydroxy-6-iodo-2-propylphenoxy)-2-hydroxypropoxy]-4-oxo-8-propyl-4H-1-benzopyran-2-carboxylic acid and its pharmaceutically acceptable salts are employed as antagonists of SRS-A (the slow reacting substance of anaphylaxis) in the treatmen
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