Design and synthesis of reboxetine analogs morpholine derivatives as selective norepinephrine reuptake inhibitors.
Bioorg Med Chem Lett
; 18(20): 5550-3, 2008 Oct 15.
Article
em En
| MEDLINE
| ID: mdl-18805691
ABSTRACT
As part of a discovery effort aimed at identifying novel norepinephrine reuptake inhibitors (NRIs), a number of substituted morpholines were designed and synthesized. The target compounds contain vicinal stereogenic centers, and the program was greatly facilitated by the adoption of efficient synthetic routes which allowed for the late stage incorporation of structural and physicochemical diversity into the targets. Structure-activity relationships were developed by optimizing individual ring components of the structure for NRI potency and for selectivity against other monoamine reuptake transporters. Several novel morpholine derivatives with a potent and selective NRI profile are described.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Norepinefrina
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Química Farmacêutica
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Morfolinas
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Inibidores da Captação Adrenérgica
Limite:
Humans
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article