New insights into homopiperazine-based 5-HT1A/5-HT7R ligands: synthesis and biological evaluation

被引:7
作者
Badarau, Eduard [4 ]
Putey, Aurelien [2 ]
Suzenet, Franck [1 ]
Joseph, Benoit [2 ]
Bojarski, Andrzej [3 ]
Finaru, Adriana [4 ]
Guillaumet, Gerald
机构
[1] Univ Orleans, Dept Chem, ICOA, F-45067 Orleans, France
[2] Univ Lyon, Lyon, France
[3] Polish Acad Sci, Krakow, Poland
[4] Univ Bacau, Fac Engn, Bacau, Romania
关键词
Homopiperazinyl; 7-azaindole; 5-HT7; 5-HT1A receptor affinity; 5-HT7 RECEPTOR LIGANDS; ANTAGONISTS; AFFINITY; CYCLASE; CLONING;
D O I
10.3109/14756360903179393
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The synthesis of new N-homopiperazinyl-based ligands is reported. Various structural modifications along with the corresponding biological activities on 5-HT1A/5-HT7 receptors give further insights into this class of serotoninergic ligands. Among the tested central heterocyles, the 7-azaindole gave the best results on the above-mentioned receptors.</.
引用
收藏
页码:301 / 305
页数:5
相关论文
共 24 条
  • [1] BARD JA, 1993, J BIOL CHEM, V268, P23422
  • [2] Pharmacophore models for metabotropic 5-HT receptor ligands
    Bojarski, Andrzej J.
    [J]. CURRENT TOPICS IN MEDICINAL CHEMISTRY, 2006, 6 (18) : 2005 - 2026
  • [3] 5-HT7 receptors in the modulation of cognitive processes
    Cifariello, Agata
    Pompili, Assunta
    Gasbarri, Antonella
    [J]. BEHAVIOURAL BRAIN RESEARCH, 2008, 195 (01) : 171 - 179
  • [4] SB-656104-A:: A novel 5-HT7 receptor antagonist with improved in vivo properties
    Forbes, IT
    Douglas, S
    Gribble, AD
    Ife, RJ
    Lightfoot, AP
    Garner, AE
    Riley, GJ
    Jeffrey, P
    Stevens, AJ
    Stean, TO
    Thomas, DR
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2002, 12 (22) : 3341 - 3344
  • [5] Functional, molecular and pharmacological advances in 5-HT7 receptor research
    Hedlund, PB
    Sutcliffe, JG
    [J]. TRENDS IN PHARMACOLOGICAL SCIENCES, 2004, 25 (09) : 481 - 486
  • [6] Novel 2-aminotetralin and 3-AminoChroman derivatives as selective serotonin 5-HT7 receptor agonists and antagonists
    Holmberg, P
    Sohn, D
    Leideborg, R
    Caldirola, P
    Zlatoidsky, P
    Hanson, S
    Mohell, N
    Rosqvist, S
    Nordvall, G
    Johansson, AM
    Johansson, R
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2004, 47 (16) : 3927 - 3930
  • [7] 1-(bicyclopiperazinyl)ethylindoles and 1-(homopiperazinyl)ethyl-indoles as highly selective and potent 5-HT7 receptor ligands
    Isaac, MB
    Xin, T
    O'Brien, A
    St-Martin, D
    Naismith, A
    MacLean, N
    Wilson, J
    Demchyshyn, L
    Tehim, A
    Slassi, A
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2002, 12 (17) : 2451 - 2454
  • [8] Joseph B, 1995, HETEROCYCLES, V41, P2769
  • [9] Tetrahydrobenzindoles:: Selective antagonists of the 5-HT7 receptor
    Kikuchi, C
    Nagaso, H
    Hiranuma, T
    Koyama, M
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (04) : 533 - 535
  • [10] Serotonin7 receptors (5-HT7Rs) and their ligands
    Leopoldo, A
    [J]. CURRENT MEDICINAL CHEMISTRY, 2004, 11 (05) : 629 - 661