- 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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- Aminoguanidine hydrazone derivatives as non-peptide NPFF1 receptor antagonists reverse opioid induced hyperalgesia
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Neuropeptide FF receptors (NPFF1R and NPFF2R) and their endogenous ligand Neuropeptide FF have been shown previously to display anti-opioid properties and to play a critical role in the adverse effects associated with chronic administrations of opiates including the development of opioid-induced hyperalgesia and analgesic tolerance. In this work, we sought to identify novel NPFF receptors ligands by focusing our interest on a series of heterocycles as rigidified non-peptide NPFF receptor ligands, starting from already described aminoguanidine hydrazones (AGH's). Binding experiments and functional assays highlighted AGH 1n and its rigidified analog 2-amino-dihydropyrimidine 22e for in vivo experiments. As earlier shown with the prototypical dipeptide antagonist RF9, both 1n and 22e reduced significantly the long lasting fentanyl-induced hyperalgesia in rodents. Altogether these data indicate that AGH rigidification maintains nanomolar affinities for both NPFF receptors, while improving antagonist character towards NPFF1R.
- Hammoud, Hassan,Elhabazi, Khadija,Quillet, Rapha?lle,Bertin, Isabelle,Utard, Valérie,Laboureyras, Emilie,Bourguignon, Jean-Jacques,Bihel, Frederic,Simonnet, Guy,Simonin, Frederic,Schmitt, Martine
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- Synthesis of 12-hetaryl-9,9-dimethyl-7,8,9,10-tetrahydrobenzo[a]acridin- 11(12H)-ones
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Three-component condensation of naphthalen-2-amine with 5-arylfuran(thiophene, N-methylpyrrole)-2-carbaldehyde and 5,5- dimethylcyclohexane-1,3-dione, as well as condensation of N-[(5- arylfuran(thiophen)-2-ylmethylidene]naphthalen-2-amine with 5,5- dimethylcyclohexane-1,3-dione gave the corresponding 12-[5-arylfuran(thiophen, N-methylpyrrol)-2-yl]-7,8,9,10-tetradrobenzo[a]acridin-11(12H)-ones.
- Kozlov,Zhikharko,Lytvyn,Gorak,Skakovskii,Baranovskii,Basalaeva,Obushak
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p. 833 - 839
(2014/08/18)
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- Synthesis and evaluation of compounds that induce readthrough of premature termination codons
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A structure-activity relationship (SAR) study was carried out to identify novel, small molecular weight compounds which induce readthrough of premature termination codons. In particular, analogs of RTC13, 1, were evaluated. In addition, hypothesizing that these compounds exhibit their activity by binding to the ribosome, we prepared the hybrid analogs 13 containing pyrimidine bases and these also showed good readthrough activity.
- Jung, Michael E.,Ku, Jin-Mo,Du, Liutao,Hu, Hailiang,Gatti, Richard A.
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supporting information; experimental part
p. 5842 - 5848
(2011/10/18)
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- Low catalyst loading ligand-free palladium-catalyzed direct arylation of furans: An economically and environmentally attractive access to 5-arylfurans
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The direct 5-arylation of furans at very low catalyst loading using Pd(OAc)2 as catalyst without added ligand proceed in high yields. Turnover numbers up to 10000 have been obtained for the coupling of several activated aryl bromides. A wide ra
- Dong, Jia Jia,Roger, Julien,Pogan, Franc,Doucet, Henri
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experimental part
p. 1832 - 1846
(2011/03/18)
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- Inhibitors of HCV NS5B polymerase. Part 1: Evaluation of the southern region of (2Z)-2-(benzoylamino)-3-(5-phenyl-2-furyl)acrylic acid
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A novel series of nonnucleoside HCV NS5B polymerase inhibitors were prepared from (2Z)-2-(benzoylamino)-3-(5-phenyl-2-furyl)acrylic acid, a high throughput screening lead. SAR studies combined with structure based drug design focusing on the southern heterobiaryl region of the template led to the synthesis of several potent and orally bioavailable lead compounds. X-ray crystallography studies were also performed to understand the interaction of these inhibitors with HCV NS5B polymerase.
- Pfefferkorn, Jeffrey A.,Greene, Meredith L.,Nugent, Richard A.,Gross, Rebecca J.,Mitchell, Mark A.,Finzel, Barry C.,Harris, Melissa S.,Wells, Peter A.,Shelly, John A.,Anstadt, Robert A.,Kilkuskie, Robert E.,Kopta, Laurice A.,Schwende, Francis J.
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p. 2481 - 2486
(2007/10/03)
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