1.
ChemMedChem
; 13(8): 795-802, 2018 04 23.
Article
in English
| MEDLINE
| ID: mdl-29451954
ABSTRACT
Selective leads: In this study, we generated a new series of serotonin 5-HT7 receptor antagonists. Their synthesis, structure-activity relationships, and selectivity profiles are reported. This series includes 5-HT7 antagonists with unprecedented high selectivity for the 5-HT7 receptor, setting the stage for lead optimization of drugs acting on a range of neurological targets.
Subject(s)
Receptors, Serotonin/metabolism , Serotonin Antagonists/chemistry , Serotonin Antagonists/pharmacology , Small Molecule Libraries/chemistry , Small Molecule Libraries/pharmacology , HEK293 Cells , Humans , Isoquinolines/chemistry , Isoquinolines/pharmacology , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 19(10): 2780-4, 2009 May 15.
Article
in English
| MEDLINE
| ID: mdl-19369077
ABSTRACT
A series of 4-azaindole inhibitors of c-Met kinase is described. The postulated binding mode was confirmed by an X-ray crystal structure and series optimisation was performed on the basis of this structure. Future directions for series development are discussed.
