Syntheses and structure-activity relationship (SAR) studies of 2,5-diazabicyclo[2.2.1]heptanes as novel α7 neuronal nicotinic receptor (NNR) ligands

被引：9
|
作者：
Li, Tao [1 ]
Bunnelle, William H. [1 ]
Ryther, Keith B. [1 ]
Anderson, David J. [1 ]
Malysz, John [1 ]
Helfrich, Rosalind [1 ]
Gronlien, Jens H. [1 ]
Hakerud, Monika [1 ]
Peters, Dan [2 ]
Schrimpf, Michael R. [1 ]
Gopalakrishnan, Murali [1 ]
Ji, Jianguo [1 ]
机构：
[1] Abbott, GPRD, Neurosci Res, Abbott Pk, IL 60064 USA
[2] NeuroSearch AS, DK-2750 Ballerup, Denmark
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 12期
关键词：
2,5-Diazabicyclo[2.2.1]heptanes; Neuronal nicotinic receptors; NNRs; alpha; 7; Cognitive deficits; ACETYLCHOLINE-RECEPTORS; DERIVATIVES; AGONISTS; BINDING;
D O I：
10.1016/j.bmcl.2010.04.105
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Biaryl substituted 2,5-diazabicyclo[2.2.1]heptanes have been synthesized and tested for their affinity toward alpha 7 neuronal nicotinic receptors (NNRs). SAR studies established that 5-N-methyl substituent, heteroaryl linker and the nature of terminal aryl group are critical for the ligand to achieve potent alpha 7 NNR agonist activity. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3636 / 3639
页数：4
相关论文
共 50 条
  • [21] Design, synthesis, insecticidal activity, and structure-activity relationship (SAR): studies of novel triazone derivatives containing a urea bridge group based on transient receptor potential (TRP) channels
    Yan Yang
    Yuxiu Liu
    Hongjian Song
    Yongqiang Li
    Qingmin Wang
    Molecular Diversity, 2016, 20 : 919 - 932
  • [22] Discovery and structure-activity relationships (SAR) of a novel class of 2-substituted N-piperidinyl indole-based nociceptin opioid receptor ligands
    Meyer, Michael E.
    Doshi, Arpit
    Polgar, Willma E.
    Zaveri, Nurulain T.
    BIOORGANIC & MEDICINAL CHEMISTRY, 2023, 92
  • [23] Design, synthesis, insecticidal activity, and structure-activity relationship (SAR): studies of novel triazone derivatives containing a urea bridge group based on transient receptor potential (TRP) channels
    Yang, Yan
    Liu, Yuxiu
    Song, Hongjian
    Li, Yongqiang
    Wang, Qingmin
    MOLECULAR DIVERSITY, 2016, 20 (04) : 919 - 932
  • [24] Model structure-activity relationship studies of potential tropane 5HT1A, 5HT2A, and D2 receptor ligands
    Slowinski, Tomasz
    Stefanowicz, Jacek
    Wrobel, Martyna Z.
    Herold, Franciszek
    Mazurek, Andrzej
    Plucinski, Franciszek
    Mazurek, Aleksander P.
    Wolska, Irena
    MEDICINAL CHEMISTRY RESEARCH, 2013, 22 (07) : 3148 - 3153
  • [25] Structure-activity relationships and molecular modeling studies of novel arylpiperazinylalkyl 2-benzoxazolones and 2-benzothiazolones as 5-HT7 and 5-HT1A receptor ligands
    Salerno, Loredana
    Pittala, Valeria
    Modica, Maria N.
    Siracusa, Maria A.
    Intagliata, Sebastiano
    Cagnotto, Alfredo
    Salmona, Mario
    Kurczab, Rafal
    Bojarski, Andrzej J.
    Romeo, Giuseppe
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2014, 85 : 716 - 726
  • [26] Structure-activity relationship studies of pyrimidine-2,4-dione derivatives as potent P2X7 receptor antagonists
    Park, Jin-Hee
    Lee, Ga-Eun
    Lee, So-Deok
    Ko, Hyojin
    Kim, Yong-Chul
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2015, 106 : 180 - 193
  • [27] Synthesis and structure-activity relationship studies of novel 2-diarylethyl substituted (2-carboxycycloprop-1-yl)glycines as high-affinity group II metabotropic glutamate receptor ligands
    Sorensen, US
    Bleisch, TJ
    Kingston, AE
    Wright, RA
    Johnson, BG
    Schoepp, DD
    Ornstein, PL
    BIOORGANIC & MEDICINAL CHEMISTRY, 2003, 11 (02) : 197 - 205
  • [28] Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists
    Nelson, Derek W.
    Gregg, Robert J.
    Kort, Michael E.
    Perez-Medrano, Arturo
    Voight, Eric A.
    Wang, Ying
    Grayson, George
    Namovic, Marian T.
    Donnelly-Roberts, Diana L.
    Niforatos, Wende
    Honore, Prisca
    Jarvis, Michael F.
    Faltynek, Connie R.
    Carroll, William A.
    JOURNAL OF MEDICINAL CHEMISTRY, 2006, 49 (12) : 3659 - 3666
  • [29] Synthesis and structure-activity relationship studies in serotonin 5-HT4 receptor ligands based on a benzo[de][2,6]naphthridine scaffold
    Castriconi, Federica
    Paolino, Marco
    Giuliani, Germano
    Anzini, Maurizio
    Campiani, Giuseppe
    Mennuni, Laura
    Sabatini, Chiara
    Lanza, Marco
    Caselli, Gianfranco
    De Rienzo, Francesca
    Menziani, Maria Cristina
    Sbraccia, Maria
    Molinari, Paola
    Costa, Tommaso
    Cappelli, Andrea
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2014, 82 : 36 - 46
  • [30] Three-dimensional quantitative structure-activity relationship CoMSIA/CoMFA and LeapFrog studies on novel series of bicyclo [4.1.0] heptanes derivatives as melanin-concentrating hormone receptor R1 antagonists
    Morales-Bayuelo, Alejandro
    Ayazo, Hernan
    Vivas-Reyes, Ricardo
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2010, 45 (10) : 4509 - 4522
12345