1.
Bioorg Med Chem Lett
; 13(19): 3277-80, 2003 Oct 06.
Article
in English
| MEDLINE
| ID: mdl-12951108
ABSTRACT
A series of substituted naphthyl containing chiral [2.2.1] bicycloheptanes were prepared utilizing asymmetric Diels-Alder chemistry. This paper describes structure-activity relationships in this series. The N-methyl 2-naphthyl analogue (16d) and its des-methyl analogue (17d) are active triple re-uptake inhibitors both in vivo and in vitro.
Subject(s)
Antidepressive Agents/chemistry , Bridged Bicyclo Compounds/chemistry , Depression/drug therapy , Neurotransmitter Uptake Inhibitors/chemistry , Animals , Antidepressive Agents/metabolism , Antidepressive Agents/therapeutic use , Binding Sites/drug effects , Binding Sites/physiology , Bridged Bicyclo Compounds/metabolism , Bridged Bicyclo Compounds/therapeutic use , Depression/metabolism , Mice , Neurotransmitter Uptake Inhibitors/metabolism , Neurotransmitter Uptake Inhibitors/therapeutic use , Synaptosomes/drug effects , Synaptosomes/metabolism
2.
Bioorg Med Chem Lett
; 12(17): 2367-70, 2002 Sep 02.
Article
in English
| MEDLINE
| ID: mdl-12161135
ABSTRACT
Several isoquinoline-based templates were identified from the studies of the conformational effects of the diketopiperazine structures for PAI-1 inhibition. Moderate to good activity was retained with the elimination of unattractive characteristics in the diketopiperazine template.
