- 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
- Zhao, Fabao,Atxabal, Unai,Mariottini, Sofia,Yi, Feng,Lotti, James S.,Rouzbeh, Nirvan,Liu, Na,Bunch, Lennart,Hansen, Kasper B.,Clausen, Rasmus P.
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p. 734 - 746
(2022/01/03)
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- Synthesis and biological evaluation of 2-phenylimino-5((5-phenylfuran-2-yl)methylene)thiazolidin-4-ones as IKK2 inhibitors
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In a search for novel molecules to treat inflammatory disorders, we identified several compounds with inhibitory action against the IKK2 enzyme using in silico methods. Based on the virtual hit of compounds 1 and 2, a novel series of 2-phenylimino-5((5-phenylfuran-2-yl)methylene)thiazolidin-4-one derivatives was designed, synthesized, and evaluated for IKK2 inhibitory activity. Among the synthesized derivatives, compounds 17f and 19f showed good IKK2 inhibitory potency, which have 4-carboxaminophenyl on the 2-furan ring and a methoxy group on the phenylimino moiety at the 2-position of the core structure. The most potent compound was 2-(2,4-dimethoxyphenyl)imino-5((5(4-carboxaminophenyl)furan-2-yl)methylene)thiazolidin-4-one (19f, IC50 = 0.94 μM), which represents a synergic effect of the two virtual hit compounds against IKK2. We also identified compounds showing inhibitory activities against interleukin (IL)-17, CCK-8, and tumor necrosis factor-alpha (TNF-α), which are NF-κB-dependent pro-inflammatory cytokine mediators.
- Kim, Hee Sook,Shin, Min Jae,Lee, Byungho,Oh, Kwang-Seok,Choo, Hyunah,Pae, Ae Nim,Roh, Eun Joo,Nam, Ghilsoo
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p. 2621 - 2626
(2015/11/16)
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- Palladium-catalyzed decarboxylative C-H bond arylation of furans
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A Pd/PCy3/Ag2CO3 (Cy = cyclohexyl) catalytic system was found to promote decarboxylative arylation through the combination of decarboxylation and C-H bond functionalization. This protocol features a good substrate scope of
- Pei, Kai,Jie, Xiaoming,Zhao, Huaiqing,Su, Weiping
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supporting information
p. 4230 - 4233
(2014/07/21)
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- A new simple route to the thieno[2,3-b]indole ring system
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A simple and effective method has been elaborated for the synthesis of thieno[2,3-b]indole ring system. It is based on the electrophilic recyclization of 2-alkyl-5-(2-isothiocyanoaryl)furans in the presence of anhydrous AlCl 3. Georg Thieme Ver
- Butin, Alexander V.,Tsiunchik, Fatima A.,Abaev, Vladimir T.,Zavodnik, Valery E.
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experimental part
p. 1145 - 1148
(2009/04/06)
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- Furan as a 1,3-diketone equivalent: the second type furan recyclization applied to indole synthesis
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A new approach for the synthesis of indole derivatives based on protolytic recyclization of 2-alkyl-5-(2-tosylaminoaryl)-furans is described. The furan ring in this unusual transformation formally serves as a 1,3-diketone equivalent.
- Butin, Alexander V.
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p. 4113 - 4116
(2007/10/03)
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