References of "Liégeois, Jean-François"
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See detailStructure du 8-chloro-11-(méthylpipérazin-1-yl)dibenzo[b,f]-1,4-thiazépine
Dupont, L.; Dideberg, O.; Liégeois, Jean-François ULg et al

in Acta Crystallographica Section C-Crystal Structure Communications (1992), C48

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See detailStructure du 6-(4-méthylpipérazin-1-yl)-11H-pyrido[2,3-b][1,4]benzodiazépine 1,5-hydrate
Dupont, L.; Englebert, S.; Dideberg, O. et al

in Acta Crystallographica Section C-Crystal Structure Communications (1992), C48

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See detailApplication de l'analyse CoMFA (Comparative Molecular Field Analysis) à une série de dérivés tricycliques apparentés à la clozapine
Liégeois, Jean-François ULg; Dupont, L.; Delarge, J.

in Journal de Pharmacie de Belgique (1992), 47

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See detailComparative study of typical neuroleptics, clozapine and newly synthesized clozapine-analogues: correlations between neurochemistry and behaviour.
Bruhwyler, J.; Liégeois, Jean-François ULg; Chleide, E. et al

in Behavioural pharmacology (1992), 3(6), 567-579

While neuroleptic therapy with classical compounds has frequently been associated with extrapyramidal side effects, clozapine has revealed an interesting antipsychotic profile without producing any ... [more ▼]

While neuroleptic therapy with classical compounds has frequently been associated with extrapyramidal side effects, clozapine has revealed an interesting antipsychotic profile without producing any clearcut motor side effects. However, some adverse reactions remained that stimulated the search for improved antipsychotic agents. The aim of this study was to characterize the behavioural and neurochemical profiles of typical neuroleptics (chlorpromazine, haloperidol), clozapine, and four newly synthesized clozapine-analogues. Affinity for dopaminergic (D1,D2), serotonergic (5-HT(2)) and cholinergic (muscarinic) receptors were measured and the ratios of these different binding affinities were determined and correlated with the behavioural effects of the drugs in a complex temporal regulation task in the dog. The four clozapine-analogues showed most of the behavioural characteristics previously described for neuroleptics and their neurochemical profile, particularly their 5-HT(2)/D2 pKi ratio, was compatible with an atypical antipsychotic effect. Among these drugs, JL5 and JL13 showed a high degree of similarity with clozapine. Like clozapine, they did not induce catalepsy and stereotypy/hyperkinesia. Moreover, other motor effects were also reduced (ataxia, akinesia, dystony). and tremor and sialorrhea were completely absent with these two molecules. [less ▲]

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See detailNew alkoxypyridine Sulfonamides: Synthesis, Biological Evaluation and Physicochemical Properties
Liégeois, Jean-François ULg; Dive, Georges ULg; Dupont, Léon et al

in Helvetica Chimica Acta (1991), 74(8), 1764-1772

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See detailStructures du 11-formyl-5-(4-méthylpipérazin-1-yl)-11H-pyrido[2,3b][1,5]benzodiazépine et du 6-(4-méthylpipérazin-1-yl)-11-méthyl-11H-pyrido[2,3-b][1,4]benzodiazépine
Dupont, L.; Englebert, S.; Dideberg, O. et al

in Acta Crystallographica Section C-Crystal Structure Communications (1991), C47

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See detailStructure du méthyl-4 pipérazinyl-1)-10 pyrido[4,3-b][1,4]benzothiazépine
Dupont, L.; Dideberg, O.; Liégeois, Jean-François ULg et al

in Acta Crystallographica Section C-Crystal Structure Communications (1991), C47

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See detailEffects of specific dopaminergic agonists and antagonists in the open-field test.
Bruhwyler, J.; Chleide, E.; Liégeois, Jean-François ULg et al

in Pharmacology, Biochemistry & Behavior (1991), 39(2), 367-71

It has been found that dopaminergic transmission could be involved in some aspects of anxiety. The present study aims to explore this hypothesis further, using specific DA1 (SKF 38393) and DA2 ... [more ▼]

It has been found that dopaminergic transmission could be involved in some aspects of anxiety. The present study aims to explore this hypothesis further, using specific DA1 (SKF 38393) and DA2 (bromocriptine) agonists or DA1 (SCH 23390), and DA2 (zetidoline) antagonists in the open-field test. The results confirm previous studies indicating that DA1 and DA2 agonists predominantly increase locomotor activity, while DA1 and DA2 antagonists predominantly decrease it. However, at low doses, the four drugs increase the peripheral ambulation score significantly and, with the exception of zetidoline, also increase the central ambulation score. The observations made with zetidoline confirm the hypothesis that a specific presynaptic DA2 antagonism could be determinant for the disinhibitory effects of low doses of neuroleptics. A collateral action on 5HT transmission is also suggested to explain an hypothetic anxiolytic action of DA agonists and SCH 23390 at lower doses. [less ▲]

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See detailStructure du N-diméthylaminoéthyl Méthoxy-4 Pyridinesulfonamide-3 et du N-[(éthyl-1pyrrolidinyl-2) méthyl] Pyridinesulfonamide-3
Dupont, L.; Dideberg, O.; Liégeois, Jean-François ULg et al

in Acta Crystallographica Section C-Crystal Structure Communications (1990), C46

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See detailAnxiolytic potential of sulpiride, clozapine and derivatives in the open-field test.
Bruhwyler, J.; Chleide, E.; Liégeois, Jean-François ULg et al

in Pharmacology, Biochemistry & Behavior (1990), 36(1), 57-61

Recently acquired data question the sharp dichotomy between anxiolytics and neuroleptics, since disinhibitory effects have been measured in the rat with very low doses of haloperidol and higher doses of ... [more ▼]

Recently acquired data question the sharp dichotomy between anxiolytics and neuroleptics, since disinhibitory effects have been measured in the rat with very low doses of haloperidol and higher doses of atypical neuroleptics in FI and DRL schedules, but also in the open-field test. That the DA transmission in certain brain regions is involved in some aspects of anxiety has recently been suggested. The present study confirms this hypothesis particularly with high doses of sulpiride (80 mg/kg) and clozapine (24 mg/kg) when tested in the open-field test. Moreover, the results show how a slight chemical modification of clozapine can give a direction to pharmacological activity with one derivative still resembling clozapine and the second one resembling haloperidol. As neuroleptics do not seem to influence the synthesis and utilization of GABA, the higher entry score observed with them would seem to depend above all on DA antagonism in the mesolimbic system. [less ▲]

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See detailStructure du (Méthyl-1-pipérazinyl-4)-5 Pyrido[2,3-b][1,5]benzothiazépine
Sbit, M.; Dupont, L.; Dideberg, O. et al

in Acta Crystallographica Section C-Crystal Structure Communications (1988), C44

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See detailStructure du N-diéthylaminoéthyl méthoxy-4 pyridine sulfonamide-3
Sbit, M.; Dupont, L.; Dideberg, O. et al

in Acta Crystallographica Section C-Crystal Structure Communications (1988), C44

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See detailStructure de la clothiapine
Sbit, M.; Dupont, L.; Dideberg, O. et al

in Acta Crystallographica Section C-Crystal Structure Communications (1987), C43

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See detailStructure du maléate de (pyrido[2,3-b]benzo-1,5-oxazépinyl-11)-4-méthyl-1H+-pipérazinium, C17H19N4OH + C4H3O4
Dupont, L.; Dideberg, O.; Liégeois, Jean-François ULg et al

in Acta Crystallographica Section C-Crystal Structure Communications (1987), C43

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See detailStructure de l'acide diphénylamino-2 carboxylique
Sbit, M.; Dupont, L.; Dideberg, O. et al

in Acta Crystallographica Section C-Crystal Structure Communications (1987), C43

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See detailAnalogues of torasemide--structure function relationships--experiments in the thick ascending limb of the loop of Henle of rabbit nephron.
Wittner, M.; Di Stefano, A.; Wangemann, P. et al

in Pflügers Archiv : European Journal of Physiology (1987), 408(1), 54-62

The aim of the present study was to examine compounds related to torasemide with respect to their ability to block the equivalent short circuit current, corresponding to the rate of chloride reabsorption ... [more ▼]

The aim of the present study was to examine compounds related to torasemide with respect to their ability to block the equivalent short circuit current, corresponding to the rate of chloride reabsorption, in isolated in vitro perfused cortical thick ascending limbs of Henle of the rabbit. The torasemide molecule was modified with respect to the anionic sulfonylurea group, and the secondary amine linked to the pyridine ring. Our results indicate that only few of the tested 48 torasemide-related compounds were able to inhibit from both epithelial sides like torasemide. Only few of the tested compounds were equally effective as torasemide from the lumen side. Some analogues were acting only from the luminal side and some only from the peritubular side. The correlations between structure and potency of inhibition from the luminal side allow the following conclusions: The secondary amine moiety linked to the pyridine ring (toluidine in case of torasemide) can be replaced by a cycloalkylamine or, with some loss of inhibitory potency, by alkylamines. The inhibitory potency is increased with the number of C-atoms in the cycloalkylamine substituted compounds (optimum C7 to C8) and is also depending on the length of the alkylamines (optimum C4). The secondary amine seems to be required since nitrogen cannot be replaced by -S- or -SO2-. The sulfonylurea group cannot be substituted by other anionic groups such as -SO-3 or -COO-. If the pyridine ring is replaced by a NO2-substituted phenyl ring, the inhibitory potency from the luminal side is lost. However, these compounds act still (with some loss of potency) from the peritubular side.(ABSTRACT TRUNCATED AT 250 WORDS) [less ▲]

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