Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics.
Bioorg Med Chem Lett
; 14(3): 585-9, 2004 Feb 09.
Article
en En
| MEDLINE
| ID: mdl-14741248
ABSTRACT
A series of (R)- and (S)-3-aminomethyl-1-tetralones, conformationally constrained analogues of haloperidol, have been obtained by enzymatic resolution of the corresponding racemic 3-hydroxymethyl-1-tetralones using Pseudomonas fluorescens lipase. Their binding affinities at dopamine D(2) and serotonin 5-HT(2A) and 5-HT(2C) receptors were determined showing in some cases an atypical antipsychotic profile with Meltzer's ratio higher than 1.30.
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Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Antipsicóticos
/
Receptores de Serotonina
/
Receptores de Dopamina D2
/
Tetralonas
/
Haloperidol
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2004
Tipo del documento:
Article
País de afiliación:
España