Synthesis and pharmacological evaluation of 3-aryl-3-azolylpropan-1-amines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors
- Bioorg Med Chem Lett. 2010 Sep 15;20(18):5567-71. doi: 10.1016/j.bmcl.2010.07.021.
Affiliations
- 1. Department of Chemistry, Korea Advanced Institute of Science and Technology, Daejeon 305-701, Republic of Korea. [email protected]
PMID: 20724153
DOI: 10.1016/j.bmcl.2010.07.021
Abstract
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.