Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Ilse, Biesmans"'
Autor:
Laura Pérez-Benito, Hilde Lavreysen, Thea Mulder-Krieger, José María Cid, Andrés A. Trabanco, Laura H. Heitman, Ilse Biesmans, Maarten L. J. Doornbos, Adriaan P. IJzerman, Gary Tresadern
Publikováno v:
British Journal of Pharmacology. 173:588-600
Background and Purpose Allosteric modulation of the mGlu 2 receptor is a potential strategy for treatment of various neurological and psychiatric disorders. Here, we describe the in vitro characterization of the mGlu 2 positive allosteric modulator (
Autor:
Paula te Riele, Gregor James Macdonald, Luc Peeters, Xavier Langlois, Wilhelmus Drinkenburg, Ilse Biesmans, José Ignacio Andrés, A. Ahnaou, Andrés A. Trabanco, Frank Matthias Dautzenberg, John R. Atack, Cindy Wintmolders, Anton Megens, Robert Johannes Lütjens, Hilde Lavreysen, José María Cid, Ilse Van der Linden
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 346:514-527
Modulation of the metabotropic glutamate type 2 (mGlu2) receptor is considered a promising target for the treatment of central nervous system diseases such as schizophrenia. Here, we describe the pharmacological properties of the novel mGlu2 receptor
Autor:
Wilhelmus Drinkenburg, Joaquín Pastor, Ilse Lenaerts, Laura Iturrino, Margot H. Bakker, Xavier Langlois, Ilse Biesmans, Jesús Alcázar, Ana Isabel de Lucas, Javier Fernández, Anton Megens, Luis M. Font, J.Ignacio Andrés, José María Cid, Rosa M. Alvarez, Shirley Pullan, Thomas Steckler, J. Alonso, Sonia Martı́nez
Publikováno v:
Bioorganic & Medicinal Chemistry. 15:3649-3660
In previous articles we have described the discovery of a new series of tricyclic isoxazolines combining central serotonin (5-HT) reuptake inhibition with alpha(2)-adrenoceptor antagonistic activity. We report now on the synthesis, the in vitro bindi
Autor:
Maarten L J, Doornbos, Laura, Pérez-Benito, Gary, Tresadern, Thea, Mulder-Krieger, Ilse, Biesmans, Andrés A, Trabanco, Jose María, Cid, Hilde, Lavreysen, Adriaan P, IJzerman, Laura H, Heitman
Publikováno v:
British journal of pharmacology. 173(3)
Allosteric modulation of the mGlu2 receptor is a potential strategy for treatment of various neurological and psychiatric disorders. Here, we describe the in vitro characterization of the mGlu2 positive allosteric modulator (PAM) JNJ-46281222 and its
Publikováno v:
The Journal of Organic Chemistry. 71:3963-3966
Assembly of the azepine ring of xantheno[9,1-cd]azepines by electrophilic cyclization of sulfonamide acetals provides access to clavizepine analogues in the form of 2,12b-dihydro- or 4-hydroxy-2,3,4,12b-tetrahydro-1H-xantheno[9,1-cd]azepines, in the
Autor:
Margot H. Bakker, Ilse Biesmans, Anton Megens, Koen A. Hens, Sonia Martı́nez, J. Alonso, Joaquín Pastor, J.Ignacio Andrés, Ana Isabel de Lucas, Ilse Lenaerts, Javier Fernández, Thomas Steckler, Laura Iturrino, Luis M. Font, Patrick C. M. Vermote, José María Cid, Jesús Alcázar, Rosa M. Alvarez
Publikováno v:
Journal of Medicinal Chemistry. 48:2054-2071
The synthesis and pharmacology of a new series of 3-piperazinylmethyl-3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles that combine central serotonin (5-HT) reuptake inhibition with alpha(2)-adrenoceptor blocking activity is described as potential ant
Autor:
Daniel Oehlrich, Encarnación Matesanz, Hilde Lavreysen, Juan Antonio Vega, María Lourdes Linares, Ana Isabel de Lucas, Gary Tresadern, José María Cid, Andrés A. Trabanco, Aránzazu García, Gregor James Macdonald, Ilse Biesmans
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(1)
Imidazo[1,2-a]pyridines were identified via their shape and electrostatic similarity as novel positive allosteric modulators of the metabotropic glutamate 2 receptor. The subsequent synthesis and SAR are described. Potent, selective and metabolically
Autor:
Jesús Alcázar, J.Ignacio Andrés, Sonia Martı́nez, Adolfo Dı́az, Javier Fernández, Ilse Biesmans, Luis M. Font, Joaquín Pastor, Celia Lafuente, Ana Isabel de Lucas, Laura Iturrino, Lieve I. Heylen, Anton Megens, Rosa M. Alvarez, José María Cid, Margot H. Bakker
Publikováno v:
Bioorganicmedicinal chemistry letters. 14(11)
In our previous paper we have described the synthesis of a series of 3-piperazinylmethyl-3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles, as novel dual 5-HT reuptake inhibitors and alpha2-adrenoceptor antagonists. That investigation led to the identi
Autor:
Sonia Martı́nez, Javier Fernández, Jesús Alcázar, Lieve I. Heylen, Rosa M. Alvarez, Ilse Biesmans, Anton Megens, Joaquín Pastor, J.Ignacio Andrés, Margot H. Bakker, Ana Isabel de Lucas, José María Cid, Carmen Nieto, J. Alonso
Publikováno v:
Bioorganicmedicinal chemistry letters. 13(16)
The synthesis of a series of novel 3-piperazinylmethyl-3a,4-dihydro-3 H -[1]benzopyrano[4,3- c ]isoxazoles as novel dual 5-HT reuptake inhibitors and α 2 -adrenoceptor antagonists is described. Their affinity at the three different human α 2 -adren
Synthesis and biological activities of conformationally restricted cyclopentenyl-glutamate analogues
Autor:
Allan H. White, Ria Wouters, Karl B. Lindsay, Alison T. Ung, Ilse Biesmans, Stephen G. Pyne, Brian W. Skelton, Ilse Van Der Linden, Kitti Amornraksa, Anne Simone Josephine Lesage, Karl Schafer
Publikováno v:
The Journal of organic chemistry. 67(1)
An efficient method for preparing conformationally restricted cyclopentenyl-glutamate analogues in a regioselective and diastereoselective manner has been developed using a formal [3 + 2] cycloaddition reaction of dehydroamino acids. Methods for prep