Identification of Triazolopyridines as Selective α5-GABAA Receptor Negative Allosteric Modulators by a Hybridization Approach.
ACS Chem Neurosci
; 14(1): 148-158, 2023 01 04.
Article
in En
| MEDLINE
| ID: mdl-36524695
ABSTRACT
The identification and characterization of novel triazolopyridine derivatives with selective α5 subunit-containing GABAA receptor negative allosteric modulator (NAM) activity are disclosed. As a result of in silico screening of our corporate compound deck, we identified a moderately potent hit that was converted to an advanced hit bearing better physicochemical and pharmacological properties using a hybridization approach. Subsequent optimization led to the identification of in vitro potent and subtype-selective α5-GABAA receptor NAMs representing a new chemotype in this area.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Receptors, GABA-A
/
Imidazoles
Type of study:
Diagnostic_studies
Language:
En
Journal:
ACS Chem Neurosci
Year:
2023
Document type:
Article
Affiliation country: