References of "Goffin, Eric"
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See detailTriphenylphosphonium salts of 1,2,4-benzothiadiazine 1,1-dioxides related to diazoxide targeting mitochondrial ATP-sensitive potassium channels
Constant-Urban, C.; Charif, M.; Goffin, Eric ULiege et al

in Bioorganic & Medicinal Chemistry Letters (2013), 23

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See detailAMPA receptor positive allosteric modulators: a patent review
Pirotte, Bernard ULiege; Francotte, Pierre ULiege; Goffin, Eric ULiege et al

in Expert Opinion on Therapeutic Patents (2013), 23

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See detailN-Aryl-N'-(chroman-4-yl)ureas and thioureas display in vitro anticancer activity and selectivity on apoptosis-resistant glioblastoma cells: screening, synthesis of simplified derivatives, and structure-activity relationship analysis.
Goffin, Eric ULiege; Lamoral-Theys, Delphine; Tajeddine, Nicolas et al

in European Journal of Medicinal Chemistry (2012), 54

A series of chroman derivatives previously reported as potassium channel openers, as well as some newly synthesized simplified structures, were examined for their in vitro effects on the growth of three ... [more ▼]

A series of chroman derivatives previously reported as potassium channel openers, as well as some newly synthesized simplified structures, were examined for their in vitro effects on the growth of three human high-grade glioma cell lines: U373, T98G, and Hs683. Significant in vitro growth inhibitory activity was observed with 2,2-dimethylchroman-type nitro-substituted phenylthioureas, such as compounds 4o and 4p. Interestingly, most tested phenylureas were found to be slightly less active, but more cell selective (normal versus tumor glial cells, such as 3d, 3e, and 3g), thus less toxic, than the corresponding phenylthioureas. No significant differences were observed in terms of chroman-derivative-induced growth inhibitory effects between glioma cells sensitive to pro-apoptotic stimuli (Hs683 glioma cells) and glioma cells associated with various levels of resistance to pro-apoptotic stimuli (U373 and T98G glioma cells), a feature that suggests non-apoptotic-mediated growth inhibition. Flow cytometry analyses confirmed the absence of pro-apoptotic effects for phenylthioureas and phenylureas when analyzed in U373 glioma cells and demonstrated U373 cell cycle arrest in the G0/G1 phase. Computer-assisted phase-contrast videomicroscopy revealed that 3d and 3g displayed cytostatic effects, while 3e displayed cytotoxic ones. As a result, this work identified phenylurea-type 2,2-dimethylchromans as a new class of antitumor agents to be further explored for an innovative therapeutic approach for high-grade glioma and/or for a possible new mechanism of action. [less ▲]

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See detailDevelopment of cognitive enhancers: design of novel thienothiadiazine 1,1-dioxides acting as AMPA potentiators
Francotte, Pierre ULiege; Goffin, Eric ULiege; Fraikin, Pierre et al

Scientific conference (2011)

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See detailNew Fluorinated 1,2,4-Benzothiadiazine 1,1-Dioxides: Discovery of an Orally Active Cognitive Enhancer Acting through Potentiation of the 2-Amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic Acid Receptors
Francotte, Pierre ULiege; Goffin, Eric ULiege; Fraikin, Pierre ULiege et al

in Journal of Medicinal Chemistry (2010), 53

In the search of a potent cognitive enhancer, a series of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides have been synthesized and evaluated as positive allosteric modulators of the AMPA receptors. In ... [more ▼]

In the search of a potent cognitive enhancer, a series of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides have been synthesized and evaluated as positive allosteric modulators of the AMPA receptors. In the present work, we focused our efforts on the insertion of mono- or polyfluoro- substituted alkyl chains at the 4-position of the thiadiazine ring in an attempt to enhance the pharmacokinetic behavior of previously described compounds. Among all the described compounds, 7-chloro-4-(2-fluoroethyl)-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide, 12b, was shown to exert a strong activity on AMPA receptors in vitro and a marked cognitive-enhancing effect in vivo after oral administration to Wistar rats. Considering its in vivo activity, the metabolic degradation of 12b was studied and compared to that of its nonfluorinated analogue 9b. Taken together, results of this study clearly validated the positive impact of the fluorine atom on the alkyl chain at the 4-position of benzothiadiazine dioxides on activity and metabolic stability. [less ▲]

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See detailDesign, synthesis, and pharmacology of novel 7-substituted 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides as positive allosteric modulators of AMPA receptors
Francotte, Pierre ULiege; De Tullio, Pascal ULiege; Goffin, Eric ULiege et al

in Journal of Medicinal Chemistry (2007), 50(13), 3153-3157

A series of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides have been synthesized and evaluated as potentiators of AMPA receptors. Attention was paid to the impact of the substituent introduced at the ... [more ▼]

A series of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides have been synthesized and evaluated as potentiators of AMPA receptors. Attention was paid to the impact of the substituent introduced at the 7-position of the heterocycle. The biological evaluation was achieved by measuring the AMPA current in rat cortex mRNA-injected Xenopus oocytes. The most potent compound, 4-ethyl-7-fluoro-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide (12a) was found to be active in an object recognition test in rats demonstrating cognition enhancing effects in vivo after oral administration. [less ▲]

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See detailProlonged unconsciousness in a patient on automated peritoneal dialysis.
Lois, Fernande ULiege; Wallemacq, Pierre; de Tourtchaninoff, Marianne et al

in European journal of emergency medicine : official journal of the European Society for Emergency Medicine (2006), 13(6), 361-3

A 79-year-old man with end-stage renal disease treated by automated peritoneal dialysis was referred to the emergency department for altered consciousness. The first investigations, including toxicology ... [more ▼]

A 79-year-old man with end-stage renal disease treated by automated peritoneal dialysis was referred to the emergency department for altered consciousness. The first investigations, including toxicology screening, failed to reveal the precise etiology. The patient was treated for a possible seizure. After the progression of central nervous system depression with bradypnea, the patient was intubated and mechanically ventilated. It appeared later on that he had ingested by mistake one of his wife's medications, baclofen. Baclofen was detected in the blood sampled on admission at a level above the therapeutic range. Baclofen is mainly excreted by the kidney. A short-term administration of low-dose of baclofen is not effectively removed by peritoneal dialysis and may result in prolonged but reversible coma. [less ▲]

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See detailIn Search of Novel Ampa Potentiators
Francotte, Pierre ULiege; De Tullio, Pascal ULiege; Fraikin, Pierre ULiege et al

in Recent Patents on CNS Drug Discovery (2006), 1(3), 239-46

Glutamate is the major excitatory neurotransmitter in the brain. Amongst ionotropic receptors responding to glutamate, the AMPA subtype has been considered as essential for the fast excitatory ... [more ▼]

Glutamate is the major excitatory neurotransmitter in the brain. Amongst ionotropic receptors responding to glutamate, the AMPA subtype has been considered as essential for the fast excitatory neurotransmission in the central nervous system and the expression and maintenance of long-term potentiation. As glutamate is known to be involved in many neurological and psychiatric disorders, AMPA receptors seem to represent interesting targets to develop therapeutic drugs. Hence, the enhancement of AMPA signals is an approach currently investigated for the management of Alzheimer's disease, schizophrenia or mood disorders. In particular, many efforts are being conducted in the development of AMPA positive allosteric modulators ("potentiators"), which alter the rate of receptor desensitization. The major chemical families developed as AMPA potentiators are aniracetam derivatives, cyclothiazide derivatives and biarylpropylsulfonamides derivatives. [less ▲]

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See detailIn vitro screening of some Strychnos species for antiplasmodial activity
Philippe, Geneviève ULiege; Angenot, Luc ULiege; De Mol, Patrick ULiege et al

in Journal of Ethnopharmacology (2005), 97(3), 535-539

The antiplasmodial activity of crude extracts of 19 species of Strychnos (Loganiaceae) was assessed in vitro against a chloroquine-susceptible strain of Plasmodium falciparum. For each species, ethyl ... [more ▼]

The antiplasmodial activity of crude extracts of 19 species of Strychnos (Loganiaceae) was assessed in vitro against a chloroquine-susceptible strain of Plasmodium falciparum. For each species, ethyl acetate (EtOAc) extracts were analysed and, for the most active species, methanolic (MeOH) extracts were also tested. Among them, Strychnos variabilis De Wild. seemed to be very promising (inhibitory concentration 50% (IC50) < 5 microg/ml) whereas two other species, Strychnos gossweileri Exell and Strychnos mellodora S. Moore, could be interesting (IC50 < 15 microg/ml) in further antimalarial studies. [less ▲]

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See detailSupercritical carbon dioxide extraction of tagitinin C from Tithonia diversifolia
Ziemons, Eric ULiege; Goffin, Eric ULiege; Lejeune, Robert ULiege et al

in Journal of Supercritical Fluids (2005), 33(1), 53-59

Different parameters as temperature, pressure, solvent mass and sample granulometry governing the extraction yield of tagitinin C from the aerial parts of Tithonia diversifolia were optimised. An ... [more ▼]

Different parameters as temperature, pressure, solvent mass and sample granulometry governing the extraction yield of tagitinin C from the aerial parts of Tithonia diversifolia were optimised. An experimental design was carried out to map the effects of pressure (at 20.3, 30.4 and 40.5 MPa) and temperature (at 40, 60 and 80degreesC) on the extraction yield of the active component and to determine the optimal conditions for the extraction of tagitinin C from T diversifolia. The best conditions are met for a pressure of 35.0 MPa and a temperature of 68degreesC. The effect of the particle size was studied under low pressure (13.7 MPa) and temperature (40degreesC) conditions, which failed to extract quantitatively the tagitinin C from leaves sieved to 250 mum size. The reduction of the particle size increased the extraction yield which became comparable to that of the optimised SFE for the particle in the range of 0-63 mum. From the analysis of extraction kinetic curves of 200 mg of plant with supercritical carbon dioxide (range of 5-30 g), it appears that 15 g of this supercritical fluid is never limiting. The optimised supercritical fluid extraction (SFE) was compared favourably to Soxhlet extraction with dichloromethane (S) and to maceration followed by lixiviation with diethyl ether (ML), which gave similar extraction yields but higher extract content of tagitinin C were found using SFE (15.6 and 30.7% w/w tagitinin C in S and ML extracts, respectively, versus 52.8% in SFE extract). [less ▲]

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