Novel pyridyl-fused 3-amino chroman derivatives with dual action at serotonin transporter and 5-HT1A receptor

被引：12
|
作者：
Zhou, Dahui
Hatzenbuhler, Nicole T.
Gross, Jonathan L.
Harrison, Boyd L.
Evrard, Deborah A.
Chlenov, Michael
Golembieski, Jeannette
Hornby, Geoffrey
Schechter, Lee E.
Smith, Deborah L.
Andree, Terrance H.
Stack, Gary P.
机构：
[1] Wyeth Ayerst Res, Chem & Screening Sci, Princeton, NJ 08543 USA
[2] Wyeth Ayerst Res, Neurosci Discovery Res, Princeton, NJ 08543 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 11期
关键词：
serotonin transporter; 5-HT1A receptor;
D O I：
10.1016/j.bmcl.2007.03.049
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Structural modifications of the initial lead, 3-aminochroman (4), led to the identification of a novel series of pyridyl-fused amino chroman derivatives (5-8) and the structural isomers (9-12). The compounds described were evaluated for dual 5-HT transporter inhibitory and 5-HT1A receptor activities. The design strategy, synthesis, and in vitro biological characterization for these novel compounds are described. (C) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3117 / 3121
页数：5
相关论文
共 50 条
  • [41] 5-HT1A receptor desensitization as mechanism underlying the lack of sexual dysfunction in female serotonin transporter knockout rats
    Snoeren, E.
    Chan, J. S. W.
    Cuppen, E.
    Olivier, B.
    Oosting, R. S.
    EUROPEAN NEUROPSYCHOPHARMACOLOGY, 2009, 19 : S52 - S53
  • [42] Adaptations in pre- and postsynaptic 5-HT1A receptor function and cocaine supersensitivity in serotonin transporter knockout rats
    Homberg, Judith R.
    De Boer, Sietse F.
    Raaso, Halfdan S.
    Olivier, Jocelien D. A.
    Verheul, Mark
    Ronken, Eric
    Cools, Alexander R.
    Ellenbroek, Bart A.
    Schoffelmeer, Anton N. M.
    Vanderschuren, Louk J. M. J.
    De Vries, Taco J.
    Cuppen, Edwin
    PSYCHOPHARMACOLOGY, 2008, 200 (03) : 367 - 380
  • [43] Studies toward the discovery of the next generation of antidepressants.: Part 5:: 3,4-Dihydro-2H-benzo[1,4]oxazine derivatives with dual 5-HT1A receptor and serotonin transporter affinity
    Zhou, DH
    Harrison, BL
    Shah, U
    Andree, TH
    Hornby, GA
    Scerni, R
    Schechter, LE
    Smith, DL
    Sullivan, KM
    Mewshaw, RE
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2006, 16 (05) : 1338 - 1341
  • [44] Is there a role for a combined mode of action of medications affecting both the 5-HT1A receptor as well as the 5-HT transporter: The clinical evidence
    Stahl, S.
    INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY, 2008, 11 : 72 - 72
  • [45] Synthesis of new arylpiperazinylalkylthiobenzimidazole, benzothiazole, or benzoxazole derivatives as potent and selective 5-HT1A serotonin receptor ligands
    Siracusa, Maria A.
    Salerno, Loredana
    Modica, Maria N.
    Pittala, Valeria
    Romeo, Giuseppe
    Amato, Maria E.
    Nowak, Mateusz
    Bojarski, Andrzej J.
    Mereghetti, Ilario
    Cagnotto, Alfredo
    Mennini, Tiziana
    JOURNAL OF MEDICINAL CHEMISTRY, 2008, 51 (15) : 4529 - 4538
  • [46] New 3-[4-(aryl)piperazin-1-yl]-1-(benzo[b]thiophen-2-yl)propane derivatives with dual action at 5-HT1A serotonin receptors and serotonin transporter as a new class of antidepressants
    Orús, L
    Sáinz, Y
    Pérez, S
    Oficialdegui, AM
    Martinez, J
    Lasheras, B
    Del Río, J
    Monge, A
    PHARMAZIE, 2002, 57 (06): : 355 - 357
  • [47] New 3-[4-(3-substiluted phenyl)piperazin-1-yl]-1-(benzo[b]thiophen-3-yl)-propanol derivatives with dual action at 5-HT1A serotonin receptors and serotonin transporter as a new class of antidepressants
    Orús, L
    Martínez, J
    Pérez, S
    Oficialdegui, AM
    Del Castillo, JC
    Mourelle, M
    Lasheras, B
    del Río, J
    Monge, A
    PHARMAZIE, 2002, 57 (08): : 515 - 518
  • [48] 13-cis-retinoic acid alters intracellular serotonin, increases 5-HT1A receptor, and serotonin Reuptake transporter levels In Vitro
    O'Reilly, Kally C.
    Trent, Simon
    Bailey, Sarah J.
    Lane, Michelle A.
    EXPERIMENTAL BIOLOGY AND MEDICINE, 2007, 232 (09) : 1195 - 1203
  • [49] Synthesis of new 5-phenyl[1,2,4]triazole derivatives as ligands for the 5-HT1A serotonin receptor
    Salerno, L
    Siracusa, M
    Guerrera, F
    Romeo, G
    Pittala, V
    Modica, M
    Mennini, T
    Russo, F
    ARKIVOC, 2004, : 312 - 324
  • [50] Identification of novel dual acting ligands targeting the adenosine A2A and serotonin 5-HT1A receptors
    Touati, Iman
    Abdalla, Mohnad
    Boulaamane, Yassir
    Al-Hoshani, Nawal
    Alouffi, Abdulaziz
    Britel, Mohammed Reda
    Maurady, Amal
    JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS, 2024, 42 (22): : 12580 - 12595
12345