Abstract
Four optical isomers of SIPI5056 were synthesized and evaluated for their antidepressant activities and acute toxicities as novel multiple reuptake inhibitors of monoamine transmitters. Chiral alanines were used as educts to prepare their respective target compounds in nine steps. Pharmacological results showed that the (1R,2S)-SIPI5056 isomer has higher inhibitory activity and lower toxicity than other three isomers and is worthy of further development.
Copyright (c) 2009 Elsevier Ltd. All rights reserved.
Publication types
-
Comparative Study
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Animals
-
Antidepressive Agents / chemical synthesis*
-
Antidepressive Agents / therapeutic use
-
Antidepressive Agents / toxicity
-
Cerebral Cortex / drug effects
-
Cerebral Cortex / metabolism
-
Lethal Dose 50
-
Mice
-
Naphthalenes / chemical synthesis*
-
Naphthalenes / therapeutic use
-
Naphthalenes / toxicity
-
Piperazines / chemical synthesis*
-
Piperazines / therapeutic use
-
Piperazines / toxicity
-
Propanols / chemical synthesis*
-
Propanols / therapeutic use
-
Propanols / toxicity
-
Rats
-
Stereoisomerism
-
Synaptosomes / drug effects
-
Synaptosomes / metabolism
Substances
-
Antidepressive Agents
-
Naphthalenes
-
Piperazines
-
Propanols