Synthesis and pharmacological evaluation of 3-aryl-3-azolylpropan-1-amines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors

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A series of 3-aryl-3-azolylpropan-1-amines was prepared and screened for its capability of inhibiting monoamine reuptake. Analogs with nanomolar potency, good human in vitro microsomal stability, and low drug-drug interaction potential were described. In vivo models were used to evaluate the compound 19r for antidepressive, anxiolytic, and analgesic activity. (C) 2010 Elsevier Ltd. All rights reserved.
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Issue Date
2010-09
Language
English
Article Type
Article
Keywords

TAIL SUSPENSION TEST; MARBLE-BURYING BEHAVIOR; SEROTONIN REUPTAKE; ANTIDEPRESSANT; MICE; BUPROPION; DOPAMINE; MODEL; COMBINATION; DISORDER

Citation

BIOORGANIC MEDICINAL CHEMISTRY LETTERS, v.20, no.18, pp.5567 - 5571

ISSN
0960-894X
DOI
10.1016/j.bmcl.2010.07.021
URI
http://hdl.handle.net/10203/98489
Appears in Collection
CH-Journal Papers(저널논문)
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