1.
Bioorg Med Chem Lett
; 14(17): 4467-70, 2004 Sep 06.
Artigo
em Inglês
| MEDLINE
| ID: mdl-15357973
RESUMO
Conformationally constrained aryl cyclohexanes and cyclohexenes based on aryl cyclohexanols 1 were prepared. Locking the aryl ring in plane with the cyclohexane moiety provided potent SSRIs 3. Conversely, fixing the aryl ring perpendicular to the cyclohexane ring via a spiro lactone provided balanced 5-HT1A antagonists with mid-nanomolar range SSRI potency (compounds 2).