Identification of Optically Active Pyrimidine Derivatives as Selective 5-HT2C Modulators.
Molecules
; 22(9)2017 Aug 26.
Article
en En
| MEDLINE
| ID: mdl-28846591
ABSTRACT
A series of pyrimidine derivatives 4a-i were synthesized and evaluated for their binding affinities towards 5-HT2C receptors. With regard to designed molecules 4a-i, the influence of the size of alkyl ether and the absolute configuration of a stereogenic center on the 5-HT2C binding affinity and selectivity was studied. The most promising diasteromeric mixtures 4d and 4e were selected in the initial radioligand binding assay and they were further synthesized as optically active forms starting from optically active alcohols 5d and 5e, prepared by an enzymatic kinetic resolution. Pyrimidine analogue (R,R)-4e displayed an excellent 5-HT2C binding affinity with good selectivity values against a broad range of other 5-HT receptor subtypes.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Pirimidinas
/
Receptor de Serotonina 5-HT2C
/
Agonistas del Receptor de Serotonina 5-HT2
Tipo de estudio:
Diagnostic_studies
Límite:
Animals
Idioma:
En
Revista:
Molecules
Asunto de la revista:
BIOLOGIA
Año:
2017
Tipo del documento:
Article