Zobrazeno 1 - 4
of 4
pro vyhledávání: '"Yves Emiel Maria Van Roosbroeck"'
Autor:
Frans A. F. Van den Keybus, Peter Jacobus Johannes Antonius Buijnsters, Andrés A. Trabanco, Marijke Somers, Marieke Lamers, Gary Tresadern, Greet Vanhoof, Yves Emiel Maria Van Roosbroeck, Gregor James Macdonald, Ingrid Velter, Philip Leonard
Publikováno v:
Journal of Medicinal Chemistry. 63:12887-12910
We describe the hit-to-lead exploration of a [1,2,4]triazolo[1,5-a]pyrimidine phosphodiesterase 2A (PDE2A) inhibitor arising from high-throughput screening. X-ray crystallography enabled structure-guided design, leading to the identification of prefe
Autor:
Garrett Berlond Minne, Michel Surkyn, Harrie J.M. Gijsen, Francois Paul Bischoff, Nigel Austin, Marc Mercken, Didier Berthelot, Chiara Zavattaro, Ishtiyaque Ahmad, Gregor James Macdonald, Adriana Ingrid Velter, Michel Anna Jozef De Cleyn, Deborah Dhuyvetter, Sven Franciscus Anna Van Brandt, Serge Maria Aloysius Pieters, Yves Emiel Maria Van Roosbroeck, Swapan Kumar Samanta, Herman Borghys
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(14)
The discovery, design and synthesis of a new series of GSMs is described. The classical imidazole heterocycle has been replaced by a cyano group attached to an indole nucleus. The exploration of this series has led to compound 26-S which combined hig
Autor:
Harrie J.M. Gijsen, Francois Paul Bischoff, Serge Maria Aloysius Pieters, Yves Emiel Maria Van Roosbroeck, Didier Berthelot, Chantal Masungi, Andrés A. Trabanco, Garrett Berlond Minne, Gary Tresadern, Adriana Ingrid Velter, Frederik J. R. Rombouts, Michel Anna Jozef De Cleyn, Libuse Jaroskova, Michel Surkyn, Tongfei Wu, Sven Franciscus Anna Van Brandt, Daniel Oehlrich, Gregor James Macdonald, Herman Borghys, Marc Mercken
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(24)
The design and synthesis of a novel series of potent gamma secretase modulators is described. Exploration of various spacer groups between the triazole ring and the aromatic appendix in 2 has led to anilinotriazole 28, which combined high in vitro an
Autor:
Andrés A. Trabanco, Meri De Angelis, Peter Jacobus Johannes Antonius Buijnsters, Wendy Sanderson, Alison Ritchie, Greet Vanhoof, Xavier Langlois, Yves Emiel Maria Van Roosbroeck, Gary Tresadern, Frederik J. R. Rombouts, José-Ignacio Andrés
Publikováno v:
ACS medicinal chemistry letters. 5(9)
Structure-guided design led to the identification of the novel, potent, and selective phosphodiesterase 2 (PDE2) inhibitor 12. Compound 12 demonstrated a >210-fold selectivity versus PDE10 and PDE11 and was inactive against all other PDE family membe