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
  • [1] Affecting AMPA Receptor Biophysical Gating Properties with Negative Allosteric Modulators
    Qneibi, Mohammad
    Hawash, Mohammad
    Jaradat, Nidal
    Bdir, Sosana
    MOLECULAR NEUROBIOLOGY, 2022, 59 (09) : 5264 - 5275
  • [2] Affecting AMPA Receptor Biophysical Gating Properties with Negative Allosteric Modulators
    Mohammad Qneibi
    Mohammad Hawash
    Nidal Jaradat
    Sosana Bdir
    Molecular Neurobiology, 2022, 59 : 5264 - 5275
  • [3] The binding site for allosteric modulators of AMPA receptor
    Tikhonova I.G.
    Lavrov M.I.
    Palyulin V.A.
    Zefirov N.S.
    Doklady Biochemistry and Biophysics, 2004, 399 (1-6) : 351 - 353
  • [4] Novel bivalent positive allosteric modulators of AMPA receptor
    Lavrov, M. I.
    Grigor'ev, V. V.
    Bachurin, S. O.
    Palyulin, V. A.
    Zefirov, N. S.
    DOKLADY BIOCHEMISTRY AND BIOPHYSICS, 2015, 464 (01) : 322 - 324
  • [5] AMPA receptor positive allosteric modulators: a patent review
    Pirotte, Bernard
    Francotte, Pierre
    Goffin, Eric
    de Tullio, Pascal
    EXPERT OPINION ON THERAPEUTIC PATENTS, 2013, 23 (05) : 615 - 628
  • [6] Computational design of positive allosteric modulators of the AMPA receptor
    Sacco, Michael
    Bonner, Lisa
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2015, 250
  • [7] Recent advances in positive allosteric modulators of the AMPA receptor
    Morrow, John A.
    Maclean, John K. F.
    Jamieson, Craig
    CURRENT OPINION IN DRUG DISCOVERY & DEVELOPMENT, 2006, 9 (05) : 571 - 579
  • [8] Novel bivalent positive allosteric modulators of AMPA receptor
    M. I. Lavrov
    V. V. Grigor’ev
    S. O. Bachurin
    V. A. Palyulin
    N. S. Zefirov
    Doklady Biochemistry and Biophysics, 2015, 464 : 322 - 324
  • [9] Tricyclic derivatives of bispidine as AMPA receptor allosteric modulators
    Lavrov, Mstislav, I
    Veremeeva, Polina N.
    Karlov, Dmitry S.
    Zamoyski, Vladimir L.
    Grigoriev, Vladimir V.
    Palyulin, Vladimir A.
    MENDELEEV COMMUNICATIONS, 2019, 29 (06) : 619 - 621
  • [10] Targeting AMPA receptor gating processes with allosteric modulators and mutations
    Mitchell, Nicholas A.
    Fleck, Mark W.
    BIOPHYSICAL JOURNAL, 2007, 92 (07) : 2392 - 2402
12345