- Derivatives of (R)-3-(5-Furanyl)carboxamido-2-aminopropanoic Acid as Potent NMDA Receptor Glycine Site Agonists with GluN2 Subunit-Specific Activity
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NMDA receptors mediate glutamatergic neurotransmission and are therapeutic targets due to their involvement in a variety of psychiatric and neurological disorders. Here, we describe the design and synthesis of a series of (R)-3-(5-furanyl)carboxamido-2-am
- Atxabal, Unai,Bunch, Lennart,Clausen, Rasmus P.,Hansen, Kasper B.,Liu, Na,Lotti, James S.,Mariottini, Sofia,Rouzbeh, Nirvan,Yi, Feng,Zhao, Fabao
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- Design, synthesis, and electrophysiological evaluation of NS6740 derivatives: Exploration of the structure-activity relationship for alpha7 nicotinic acetylcholine receptor silent activation
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The α7 nicotinic acetylcholine receptor (nAChR) silent agonists, able to induce receptor desensitization and promote the α7 metabotropic function, are emerging as new promising therapeutic anti-inflammatory agents. Herein, we report the structure–activity
- Pismataro, Maria Chiara,Horenstein, Nicole A.,Stokes, Clare,Quadri, Marta,De Amici, Marco,Papke, Roger L.,Dallanoce, Clelia
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- Small-molecular inhibitors of Ca2+-induced mitochondrial permeability transition (MPT) derived from muscle relaxant dantrolene
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A structure consisting of substituted hydantoin linked to a 5-(halophenyl)furan-2-yl group via an amide bond was identified as a promising scaffold for development of low-molecular-weight therapeutic agents to treat vascular dysfunction, including ischemia/reperfusion injury. Among the compounds synthesized, 5-(3,5-dichlorophenyl)-N-{2,4-dioxo-3-[(pyridin-3-yl)methyl] imidazolidin-1-yl}-2-furamide (17) possessed the most potent inhibitory activity against Ca2+-induced mitochondrial swelling. The structural development, synthesis and structure-activity relationship of these compounds are described.
- Murasawa, Shinpei,Sato, Shinichi,Noguchi-Yachide, Tomomi,Hashimoto, Yuichi,Iuchi, Katsuya,Sodeoka, Mikiko,Dodo, Kosuke,Yokomatsu, Tsutomu,Aoyama, Hiroshi
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p. 6384 - 6393,10
(2012/12/11)
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- Synthesis of heterocycles from arylation products of unsaturated compounds: XVIII. 5-Arylfuran-2-carboxylic acids and their application in the synthesis of 1,2,4-thiadiazole, 1,3,4-oxadiazole, and [1,2,4]triazolo[3,4-b][1,3,4] thiadiazole derivatives
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Arylation of furan-2-carboxylic acid or its methyl ester with arenediazonium chlorides in the presence of copper(II) chloride gave the corresponding 5-arylfuran-2-carboxylic acids or methyl 5-arylfuran-2- carboxylates. 5-Arylfuran-2-carbonyl chlorides rea
- Gorak,Obushak,Matiichuk,Lytvyn
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experimental part
p. 541 - 550
(2009/08/17)
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- Synthesis of some thiadiazolotriazinone derivatives as possible antimicrobial agents
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A series of 7-substituted-3-t-butyl 4(H)-1,3,4-thiadiazolo(2,3-c)-1,2,4- triazine-4-one (3) have been synthesized by condensing 4-amino-6-t-butyl-3- mercapto-1,2,4-triazin-5(4H)-one (1) with substituted Arylfuroic acids (2) using POCl3 as a cyclizing agen
- Prasad, D. Jagadeesh,Karthikeyan,Karegoudar, Prakash B.,Poojary, Boja,Holla, B. Shivarama,Kumari, N. Suchetha
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p. 1083 - 1091
(2008/02/01)
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