Search Results - "Carrupt, P"

Stereoselective Block of hERG Channel by ( )-Methadone and QT Interval Prolongation in CYP2B6 Slow Metabolizers by Eap, C B, Crettol, S, Rougier, J‐S, Schläpfer, J, Sintra Grilo, L, Déglon, J‐J, Besson, J, Croquette‐Krokar, M, Carrupt, P‐A, Abriel, H

“…Methadone inhibits the cardiac potassium channel hERG and can cause a prolonged QT interval. Methadone is chiral but its therapeutic activity is mainly due to…”
Get full text

QSAR analysis and molecular modeling of ABCG2-specific inhibitors by Nicolle, E., Boumendjel, A., Macalou, S., Genoux, E., Ahmed-Belkacem, A., Carrupt, P.-A., Di Pietro, A.

“…In addition to its critical role is controlling drug availability and protecting sensitive organs and stem cells through cellular detoxification, breast cancer…”
Get full text

Targeting the multidrug ABCG2 transporter with flavonoidic inhibitors: in vitro optimization and in vivo validation by Boumendjel, A, Macalou, S, Valdameri, G, Pozza, A, Gauthier, C, Arnaud, O, Nicolle, E, Magnard, S, Falson, P, Terreux, R, Carrupt, P-A, Payen, L, Di Pietro, A

“…This review describes the breast cancer resistance protein ABCG2 through its structure, functional roles and involvement in cell multidrug resistance,…”
Get more information

Predicting Blood−Brain Barrier Permeation from Three-Dimensional Molecular Structure by Crivori, Patrizia, Cruciani, Gabriele, Carrupt, Pierre-Alain, Testa, Bernard

“…Predicting blood−brain barrier (BBB) permeation remains a challenge in drug design. Since it is impossible to determine experimentally the BBB partitioning of…”
Get full text

Xanthones from Gentianella amarella ssp. acuta with Acetylcholinesterase and Monoamine Oxidase Inhibitory Activities by Urbain, A., Marston, A., Grilo, L. Sintra, Bravo, J., Purev, O., Purevsuren, B., Batsuren, D., Reist, M., Carrupt, P.-A., Hostettmann, K.

“…Two new xanthone glycosides, corymbiferin 3-O-β-d-glucopyranoside (1) and swertiabisxanthone-I 8′-O-β-d-glucopyranoside (2), were isolated from Gentianella…”
Get full text

Coumarins Derivatives as Dual Inhibitors of Acetylcholinesterase and Monoamine Oxidase by Brühlmann, Corinne, Ooms, Frédéric, Carrupt, Pierre-Alain, Testa, Bernard, Catto, Marco, Leonetti, Francesco, Altomare, Cosimo, Carotti, Angelo

“…A set of 17 coumarin and 2 chromone derivatives with known inhibitory activity toward monoamine oxidase (MAO) A and B were tested as acetylcholinesterase…”
Get full text

Inhibition of Monoamine Oxidases by Functionalized Coumarin Derivatives:  Biological Activities, QSARs, and 3D-QSARs by Gnerre, Carmela, Catto, Marco, Leonetti, Francesco, Weber, Peter, Carrupt, Pierre-Alain, Altomare, Cosimo, Carotti, Angelo, Testa, Bernard

“…A large series of coumarin derivatives (71 compounds) were tested for their monoamine oxidase A and B (MAO-A and MAO-B) inhibitory activity. Most of the…”
Get full text

Anti-inflammatory, antimicrobial and antioxidant activities of Diospyros bipindensis (Gürke) extracts and its main constituents by Cesari, I., Hoerlé, M., Simoes-Pires, C., Grisoli, P., Queiroz, E.F., Dacarro, C., Marcourt, L., Moundipa, P.F., Carrupt, P.A., Cuendet, M., Caccialanza, G., Wolfender, J.L., Brusotti, G.

“…Diospyros bipindensis (Gürke) stem bark is used in Cameroon by Baka Pygmies for the treatment of respiratory disorders. To assess the anti-inflammatory,…”
Get full text

Antioxidant potential and radical-scavenging effects of flavonoids from the leaves of Psidium cattleianum grown in French Polynesia by Ho, R., Violette, A., Cressend, D., Raharivelomanana, P., Carrupt, P.A., Hostettmann, K.

“…Psidium cattleianum J. Sabine (Myrtaceae) is a traditional medicinal plant in French Polynesia. The leaves and roots possess many medicinal properties. These…”
Get full text

Antifungals and acetylcholinesterase inhibitors from the stem bark of Croton heliotropiifolius by Queiroz, M.M.F., Queiroz, E.F., Zeraik, M.L., Marti, G., Favre-Godal, Q., Simões-Pires, C., Marcourt, L., Carrupt, P.A., Cuendet, M., Paulo, M.Q., Bolzani, V.S., Wolfender, J.L.

“…•C. heliotropiifolius EtOH extract showed antifungal and AChE inhibitory activities.•Dereplication and localization of active constituents was performed by…”
Get full text

Generalization of Ionic Partition Diagrams to Lipophilic Compounds and to Biphasic Systems with Variable Phase Volume Ratios by Gobry, Véronique, Ulmeanu, Sorina, Reymond, Frédéric, Bouchard, Géraldine, Carrupt, Pierre-Alain, Testa, Bernard, Girault, Hubert H

“…The ionic partition diagram methodology has been generalized to address both hydrophilic and lipophilic compounds and to consider biphasic systems with…”
Get full text

Chiral Inversion and Hydrolysis of Thalidomide:  Mechanisms and Catalysis by Bases and Serum Albumin, and Chiral Stability of Teratogenic Metabolites by Reist, Marianne, Carrupt, Pierre-Alain, Francotte, Eric, Testa, Bernard

“…The chiral inversion and hydrolysis of thalidomide and the catalysis by bases and human serum albumin were investigated by using a stereoselective HPLC assay…”
Get full text

Isoquinoline derivatives as endogenous neurotoxins in the aetiology of Parkinson’s disease by McNaught, Kevin St.P., Carrupt, Pierre-Alain, Altomare, Cosimo, Cellamare, Saverio, Carotti, Angelo, Testa, Bernard, Jenner, Peter, Marsden, C.David

“…The cause of neurodegeneration in Parkinson’s disease (PD) remains unknown. However, isoquinoline derivatives structurally related to the selective…”
Get full text

Fast determination of lipophilicity by HPLC by AYOUNI, L, CAZORLA, G, CHAILLOU, D, HERBRETEAU, B, RUDAZ, S, LANTERI, P, CORRUPT, P.-A

Get full text

Inhibition of Monoamine Oxidase-B by Condensed Pyridazines and Pyrimidines:  Effects of Lipophilicity and Structure−Activity Relationships by Altomare, Cosimo, Cellamare, Saverio, Summo, Luciana, Catto, Marco, Carotti, Angelo, Thull, Ulrike, Carrupt, Pierre-Alain, Testa, Bernard, Stoeckli-Evans, Helen

“…A number of condensed pyridazines and pyrimidines were synthesized and tested for their monoamine oxidase-A (MAO-A) and MAO-B inhibitory activity. Their…”
Get full text

Lipophilicity in molecular modeling by TESTA, B, CARRUPT, P.-A, GAILLARD, P, BILLOIS, F, WEBER, P

“…The molecular lipophilicity potential (MLP) offers a three-dimensional representation of lipophilicity, a molecular property encoding intermolecular…”
Get full text

Evaluation and Prediction of Drug Permeation by PAGLIARA, ALESSANDRA, REIST, MARIANNE, GEINOZ, SANDRINE, CARRUPT, PIERRE-ALAIN, TESTA, BERNARD

“…A major challenge confronting the pharmaceutical scientist is to optimize the selective and efficient delivery of new active entities and drug candidates…”
Get full text

Molecular Properties and Pharmacokinetic Behavior of Cetirizine, a Zwitterionic H1-Receptor Antagonist by Pagliara, Alessandra, Testa, Bernard, Carrupt, Pierre-Alain, Jolliet, Pascale, Morin, Christophe, Morin, Didier, Urien, Saïk, Tillement, Jean-Paul, Rihoux, Jean-Pierre

“…The ionization and lipophilicity behavior of the antihistamine (H1-receptor antagonist) cetirizine was investigated, showing the drug to exist almost…”
Get full text

Inhibition of monoamine oxidase by isoquinoline derivatives: Qualitative and 3D-quantitative structure-activity relationships by Thull, Ulrike, Kneubühler, Silvia, Gaillard, Patrick, Carrupt, Pierre-Alain, Testa, Bernard, Altomare, Cosimo, Carotti, Angelo, Jenner, Peter, St. P. McNaught, Kevin

“…A series of isoquinolines, N-methyl-1,2-dihydroisoquinolines, N-methyl-1,2,3,4-tetrahydroisoquinolines, 1,2,3,4-tetrahydroisoquinolines, and…”
Get full text

Structural damage to proteins caused by free radicals: asessment, protection by antioxidants, and influence of protein binding by Salvi, Aline, Carrupt, Pierre-Alain, Tillement, Jean-Paul, Testa, Bernard

“…Oxidative damage to proteins results in biological dysfunctions such as perturbed activity in enzymes, transport proteins, and receptors. Here, we investigated…”
Get full text