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
来源：
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2010年 / 25卷 / 03期
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 50 条
  • [41] Design, Synthesis, and Biological Evaluation of a Series of 5- and 7-Hydroxycoumarin Derivatives as 5-HT1A Serotonin Receptor Antagonists
    Ostrowska, Kinga
    Lesniak, Anna
    Czarnocka, Zuzanna
    Chmiel, Jagoda
    Bujalska-Zadrozny, Magdalena
    Trzaskowski, Bartosz
    PHARMACEUTICALS, 2021, 14 (03) : 1 - 30
  • [42] PHYSIOLOGICAL-EFFECTS OF SELECTIVE 5-HT1A AND 5-HT1B LIGANDS IN RAT HIPPOCAMPUS - COMPARISON TO 5-HT
    SEGAL, M
    AZMITIA, EC
    WHITAKERAZMITIA, PM
    BRAIN RESEARCH, 1989, 502 (01) : 67 - 74
  • [43] Design and synthesis of potent and selective 5-HT1A receptor ligands.
    Zhang, G
    Palmer, Y
    Kelly, MG
    Smith, DL
    Schechter, LE
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2000, 220 : U557 - U557
  • [44] Receptor-based pharmacophores for serotonin 5-HT7R antagonists -: Implications to selectivity
    Kolaczkowski, Marcin
    Nowak, Mateusz
    Pawlowski, Maciej
    Bojarski, Andrzej J.
    JOURNAL OF MEDICINAL CHEMISTRY, 2006, 49 (23) : 6732 - 6741
  • [45] Arylpiperazine derivatives of 3-propyl-β-tetralonohydantoin as new 5-HT1A and 5-HT2A receptor ligands
    Byrtus, H
    Pawlowski, M
    Duszynska, B
    Wesolowska, A
    Chojnacka-Wójcik, E
    Bojarski, AJ
    POLISH JOURNAL OF PHARMACOLOGY, 2001, 53 (04): : 395 - 401
  • [46] An Algorithm to Identify Target-Selective Ligands - A Case Study of 5-HT7/5-HT1A Receptor Selectivity
    Kurczab, Rafal
    Canale, Vittorio
    Zajdel, Pawel
    Bojarski, Andrzej J.
    PLOS ONE, 2016, 11 (06):
  • [47] Computational Methods in Determination of Pharmacophore Models of 5-HT1A, 5-HT2A and 5-HT7 Receptors
    Bielenica, Anna
    Koziol, Anna E.
    Struga, Marta
    MINI-REVIEWS IN MEDICINAL CHEMISTRY, 2013, 13 (07) : 933 - 951
  • [48] Ultrasound assisted one-pot synthesis and preliminary in vitro studies of salicylamide arylpiperazines as dual 5-HT1A/5-HT7 ligands
    Jaskowska, Jolanta
    Drabczyk, Anna Karolina
    Sliwa, Pawel
    Jodlowski, Przemyslaw
    Pindelska, Edyta
    Kulaga, Damian
    Zareba, Przemyslaw
    Majka, Zbigniew
    Siwek, Agata
    Wolak, Malgorzata
    Kolaczkowski, Marcin
    JOURNAL OF MOLECULAR STRUCTURE, 2023, 1275
  • [49] 5-HT1A receptor ligands and their therapeutic applications: review of new patents
    Staron, Jakub
    Bugno, Ryszard
    Hogendorf, Adam S.
    Bojarski, Andrzej J.
    EXPERT OPINION ON THERAPEUTIC PATENTS, 2018, 28 (09) : 679 - 689
  • [50] COMPUTATIONAL METHODS IN DETERMINATION OF PHARMACOPHORE MODELS OF 5-HT1A, 5-HT2A AND 5-HT7 RECEPTORS
    Bielenica, Anna
    Kossakowski, Jerzy
    BIULETYN WYDZIALU FARMACEUTYCZNEGO WARSZAWSKIEGO UNIWERSYTETU MEDYCZNEGO, 2010, (01): : 1 - 12
12345