QSAR study of anticonvulsant negative allosteric modulators of the AMPA receptor

被引：18
|
作者：
Macchiarulo, A
De Luca, L
Costantino, G
Barreca, ML
Gitto, R
Pellicciari, R
Chimirri, A
机构：
[1] Univ Messina, Dipartimento Farmacochim, I-98168 Messina, Italy
[2] Univ Perugia, Dipartimento Chim & Tecnol Farmaco, I-06123 Perugia, Italy
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2004年 / 47卷 / 07期
关键词：
D O I：
10.1021/jm0310838
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A quantitative structure-activity relationship (QSAR) study was performed on a set of 49 negative allosteric modulators of AMPA receptor, acting as anticonvulsant agents, using multiple linear regression. The predictive ability of the resulting model was evaluated against a set of 12 compounds; the results showed good statistics in regression and revealed high correlation between anticonvulsant activity and some electrotopological descriptors.
引用
收藏
页码：1860 / 1863
页数：4
相关论文
共 50 条
  • [41] Mechanism of positive allosteric modulators acting on AMPA receptors
    Jin, RS
    Clark, S
    Weeks, AM
    Dudman, JT
    Gouaux, E
    Partin, KM
    JOURNAL OF NEUROSCIENCE, 2005, 25 (39): : 9027 - 9036
  • [42] A novel class of allosteric modulators of AMPA/Kainate receptors
    Cannazza, Giuseppe
    Jozwiak, Krzysztof
    Parenti, Carlo
    Braghiroli, Daniela
    Carrozzo, Marina M.
    Puia, Giulia
    Losi, Gabriele
    Baraldi, Mario
    Lindner, Wolfgang
    Wainer, Irving W.
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2009, 19 (04) : 1254 - 1257
  • [43] Pharmacophore analysis of positive allosteric modulators of AMPA receptors
    Karlov, D. S.
    Lavrov, M. I.
    Palyulin, V. A.
    Zefirov, N. S.
    RUSSIAN CHEMICAL BULLETIN, 2016, 65 (02) : 581 - 587
  • [44] Computer-aided design of negative allosteric modulators of NMDA receptor
    E. V. Radchenko
    D. S. Karlov
    A. N. Zefirov
    V. A. Palyulin
    N. S. Zefirov
    V. M. Pentkovski
    Doklady Biochemistry and Biophysics, 2013, 448 : 22 - 26
  • [45] Computer-aided design of negative allosteric modulators of NMDA receptor
    Radchenko, E. V.
    Karlov, D. S.
    Zefirov, A. N.
    Palyulin, V. A.
    Zefirov, N. S.
    Pentkovski, V. M.
    DOKLADY BIOCHEMISTRY AND BIOPHYSICS, 2013, 448 (01) : 22 - 26
  • [46] Design of negative allosteric modulators of the dopamine D2 receptor
    Mishra, Satyendra
    Bhagwanth, Swapna
    Daya, Ritesh P.
    Mah, Jordan K.
    Mishra, Ram K.
    Johnson, Rodney L.
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2011, 242
  • [47] Pyrimidine derivatives as mGlu5 receptor negative allosteric modulators
    Li, Guiying
    April, Myriam
    Pu, Xiaosui
    Uberti, Michelle A.
    Brodbeck, Robbin M.
    Bacolod, Maria D.
    Chandrasena, Gamini
    Doller, Dario
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2014, 248
  • [48] Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor
    Burford, Neil T.
    Clark, Mary J.
    Wehrman, Tom S.
    Gerritz, Samuel W.
    Banks, Martyn
    O'Connell, Jonathan
    Traynor, John R.
    Alt, Andrew
    PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 2013, 110 (26) : 10830 - 10835
  • [49] AMPA receptor-positive allosteric modulators for the treatment of schizophrenia: an overview of recent patent applications
    Ward, Simon E.
    Pennicott, Lewis E.
    Beswick, Paul
    FUTURE MEDICINAL CHEMISTRY, 2015, 7 (04) : 473 - 491
  • [50] Functional insight into development of positive allosteric modulators of AMPA receptors
    Weeks, Autumn M.
    Harms, Jonathan E.
    Partin, Kathryn M.
    Benveniste, Morris
    NEUROPHARMACOLOGY, 2014, 85 : 57 - 66
12345