Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists

被引：5
|
作者：
Stark, H
Ligneau, X
Sadek, B
Ganellin, CR
Arrang, JM
Schwartz, JC
Schunack, W
机构：
[1] Free Univ Berlin, Inst Pharm, D-14195 Berlin, Germany
[2] Lab Bioprojet, F-75003 Paris, France
[3] UCL, Christopher Ingold Labs, London WC1H 0AJ, England
[4] INSERM, Unite Neurobiol & Pharmacol Mol, U109, F-75014 Paris, France
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 20期
关键词：
D O I：
10.1016/S0960-894X(00)00473-X
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Novel derivatives of the highly potent and selective histamine H-3-receptor antagonist ciproxifan (3) with different chain lengths as well as with structural variants of the cyclopropyl ketone moiety have been prepared and screened for their antagonist H3-receptor potencies in vitro and in vivo. Some derivatives (2, 6-8, 12) containing other functionalities were effective in vitro in the same (sub)nanomolar concentration range and in vivo in a remarkably low oral dose. (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：2379 / 2382
页数：4
相关论文
共 50 条
  • [1] Ciproxifan and chemically related compounds are highly potent and selective histamine H3-receptor antagonists
    M. Kathmann
    E. Schlicker
    I. Marr
    S. Werthwein
    H. Stark
    W. Schunack
    [J]. Naunyn-Schmiedeberg's Archives of Pharmacology, 1998, 358 : 623 - 627
  • [2] Ciproxifan and chemically related compounds are highly potent and selective histamine H3-receptor antagonists
    Kathmann, M
    Schlicker, E
    Marr, L
    Werthwein, S
    Stark, H
    Schunack, W
    [J]. NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 1998, 358 (06) : 623 - 627
  • [3] Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist
    Ligneau, X
    Lin, JS
    Vanni-Mercier, G
    Jouvet, M
    Muir, JL
    Ganellin, CR
    Stark, H
    Elz, S
    Schunack, W
    Schwartz, JC
    [J]. JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 1998, 287 (02): : 658 - 666
  • [4] Theophylline derivatives as potential histamine H3-receptor antagonists
    Kiec-Kononowicz, K
    Cegla, MT
    [J]. PHARMAZIE, 1998, 53 (08): : 518 - 521
  • [5] Convenient procedures for synthesis of ciproxifan, a histamine H3-receptor antagonist
    Stark, H
    [J]. ARCHIV DER PHARMAZIE, 2000, 333 (09) : 315 - 316
  • [6] The discovery of potent non-imidazole H3-receptor histamine antagonists
    Ganellin, CR
    Leurquin, F
    Piripitsi, A
    Arrang, JM
    Garbarg, M
    Ligneau, X
    Stark, H
    Schunack, W
    Schwartz, JC
    [J]. HISTAMINE RESEARCH IN THE NEW MILLENNIUM, 2001, 1224 : 25 - 31
  • [7] Molecules -: Histamine H3-receptor antagonists
    Lloyd, AW
    [J]. DRUG DISCOVERY TODAY, 1999, 4 (12) : 568 - 568
  • [8] Synthesis of potent non-imidazole histamine H3-receptor antagonists
    Ganellin, CR
    Leurquin, F
    Piripitsi, A
    Arrang, JM
    Garbarg, M
    Ligneau, X
    Schunack, W
    Schwartz, JC
    [J]. ARCHIV DER PHARMAZIE, 1998, 331 (12) : 395 - 404
  • [9] Progress in the proxifan class:: heterocyclic congeners as novel potent and selective histamine H3-receptor antagonists
    Grassmann, S
    Sadek, B
    Ligneau, X
    Elz, S
    Ganellin, CR
    Arrang, JM
    Schwartz, JC
    Stark, H
    Schunack, W
    [J]. EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2002, 15 (04) : 367 - 378
  • [10] Benzophenone derivatives and related compounds as potent histamine H3-receptor antagonists and potential PET/SPECT ligands
    Sasse, A
    Ligneau, X
    Sadek, B
    Elz, S
    Pertz, HH
    Ganellin, CR
    Arrang, JM
    Schwartz, JC
    Schunack, W
    Stark, H
    [J]. ARCHIV DER PHARMAZIE, 2001, 334 (02) : 45 - 52
12345