Synthesis, structure-activity relationship studies, and identification of novel 5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 1.
Bioorg Med Chem Lett
; 23(7): 2212-6, 2013 Apr 01.
Article
in En
| MEDLINE
| ID: mdl-23434414
ABSTRACT
A novel series of non-peptidic OX1R/OX2R orexin receptor antagonists was prepared by heterocyclic replacement of the dimethoxyphenyl moiety contained in the tetrahydroisoquinoline core skeleton of almorexant. Introduction of substituted imidazole moieties delivered potent dual orexin receptor antagonists with nanomolar potency for hOX1R and hOX2R suitable for further fine-tuning. The preparation of these novel orexin receptor antagonists and the outcome of preliminary structure-activity relationship studies are described in this communication.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Pyrazines
/
Receptors, Neuropeptide
/
Receptors, G-Protein-Coupled
Type of study:
Diagnostic_studies
Limits:
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Year:
2013
Document type:
Article