title: Synthesis and pharmacological evaluation of 3-aryl-3-azolylpropan-1-amines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors.
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.
authors: Department of Chemistry, Korea Advanced Institute of Science and Technology, Daejeon 305-701, Republic of Korea. kiho.lee@sk.com
authors: Ki-Ho
authors: KH
authors: Lee
authors: Chun-Eung
authors: CE
authors: Park
authors: Kyung-Hyun
authors: KH
authors: Min
authors: Yong-Je
authors: YJ
authors: Shin
authors: Coo-Min
authors: CM
authors: Chung
authors: Hui-Ho
authors: HH
authors: Kim
authors: Hae-Jeoung
authors: HJ
authors: Yoon
authors: Won-Kim
authors: Eun-Ju
authors: EJ
authors: Ryu
authors: Yu-Jin
authors: YJ
authors: Shin
authors: Hyun-Sik
authors: HS
authors: Nam
authors: Jeong-Woo
authors: JW
authors: Cho
authors: Hee-Yoon
authors: HY
authors: Lee
mesh_terms: D000700:Analgesics / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D014151:Anti-Anxiety Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D000928:Antidepressive Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D016466:CHO Cells; D002460:Cell Line; D006224:Cricetinae; D003412:Cricetulus; D004298:Dopamine / Q000378:metabolism*; D006801:Humans; D051379:Mice; D014179:Neurotransmitter Uptake Inhibitors / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D009638:Norepinephrine / Q000378:metabolism*; D011437:Propylamines / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D051381:Rats; D012701:Serotonin / Q000378:metabolism*; D013777:Tetrazoles / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*
chemical_list: D000700:Analgesics; D014151:Anti-Anxiety Agents; D000928:Antidepressive Agents; D014179:Neurotransmitter Uptake Inhibitors; D011437:Propylamines; D013777:Tetrazoles; D012701:Serotonin; D004298:Dopamine; D009638:Norepinephrine