Design and development of 2,3-benzodiazepine (CFM) noncompetitive AMPA receptor antagonists

被引：25
作者：
Gitto, R
Zappalà, M
De Sarro, G
Chimirri, A
机构：
[1] Univ Messina, Dipartimento Farmacochim, I-98168 Messina, Italy
[2] Univ Magna Groecia Catanzaro, Dipartimento Med Sperimentale & Clin, Catedra Farmacol, I-88100 Catanzaro, Italy
来源：
FARMACO | 2002年 / 57卷 / 02期
关键词：
AMPA-antagonists; 2,3-benzodiazepines; anticonvulsant agents;
D O I：
10.1016/S0014-827X(01)01186-7
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
2,3-Benzodiazepines represent a class of heterocyclic compounds that interact with AMPA-type glutamate receptors in a noncompetitive manner. These compounds have attracted great interest for their pharmacological effects against acute and chronic neurodegenerative diseases, such as ischemia and epilepsy. We synthesized a large number of 2,3-benzodiazepine derivatives, which showed anticonvulsant properties in different seizure models and a noncompetitive blockade of AMPA receptor. This article will briefly mention our work in this field and the main SAR considerations. (C) 2002 Editions scientifiques et medicales Elsevier SAS. All rights reserved.
引用
收藏
页码：129 / 134
页数：6
相关论文
共 32 条
  • [1] Activity of 2,3-benzodiazepines at native rat and recombinant human glutamate receptors in vitro: Stereospecificity and selectivity profiles
    Bleakman, D
    Ballyk, BA
    Schoepp, DD
    Palmer, AJ
    Bath, CP
    Sharpe, EF
    Woolley, ML
    Bufton, HR
    Kamboj, RK
    Tarnawa, I
    Lodge, D
    [J]. NEUROPHARMACOLOGY, 1996, 35 (12) : 1689 - 1702
  • [2] ANIRACETAM REVERSES THE ANTICONVULSANT ACTION OF NBQX AND GYKI 52466 IN DBA/2 MICE
    CHAPMAN, AG
    ALZUBAIDY, Z
    MELDRUM, BS
    [J]. EUROPEAN JOURNAL OF PHARMACOLOGY, 1993, 231 (02) : 301 - 303
  • [3] 3,5-dihydro-4H-2,3-benzodiazepine-4-thiones:: A new class of AMPA receptor antagonists
    Chimirri, A
    De Sarro, G
    De Sarro, A
    Gitto, R
    Quartarone, S
    Zappalà, M
    Constanti, A
    Libri, V
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1998, 41 (18) : 3409 - 3416
  • [4] Synthesis and structural features of 11H-tetrazolo[1,5-c] [2,3]benzodiazepines
    Chimirri, A
    Zappalà, M
    Gitto, R
    Quartarone, S
    Bevacqua, F
    [J]. HETEROCYCLES, 1999, 51 (06) : 1303 - +
  • [5] AMPA receptor antagonists
    Chimirri, A
    Gitto, R
    Zappalà, M
    [J]. EXPERT OPINION ON THERAPEUTIC PATENTS, 1999, 9 (05) : 557 - 570
  • [6] 1-aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: Novel AMPA receptor antagonists
    Chimirri, A
    DeSarro, G
    DeSarro, A
    Gitto, R
    Grasso, S
    Quartarone, S
    Zappala, M
    Giusti, P
    Libri, V
    Constanti, A
    Chapman, AG
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1997, 40 (08) : 1258 - 1269
  • [7] Chimirri A, 1999, MED CHEM RES, V9, P203
  • [8] Anticonvulsant activity and plasma level of 2,3-benzodiazepin-4-ones (CFMs) in genetically epilepsy-prone rats
    De Sarro, G
    Rizzo, M
    Spagnolo, C
    Gitto, R
    De Sarro, A
    Scotto, G
    Zappala, M
    Chimirri, A
    [J]. PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR, 1999, 63 (04) : 621 - 627
  • [9] Relationship between anticonvulsant activity and plasma level of some 2,3-benzodiazepines in genetically epilepsy-prone rats
    DE Sarro, G
    Rizzo, M
    Sinopoli, VA
    Gitto, R
    DE Sarro, A
    Zappala, M
    Chimirri, A
    [J]. PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR, 1998, 61 (03) : 215 - 220
  • [10] GYKI 52466 and related 2,3-benzodiazepines as anticonvulsant agents in DBA/2 mice
    DeSarro, G
    Chimirri, A
    DeSarro, A
    Gitto, R
    Grasso, S
    Giusti, P
    Chapman, AG
    [J]. EUROPEAN JOURNAL OF PHARMACOLOGY, 1995, 294 (2-3) : 411 - 422
1234