Structure-activity relationships of arylbenzofuran H3 receptor antagonists

被引:50
作者
Gfesser, GA [1 ]
Faghih, R [1 ]
Bennani, YL [1 ]
Curtis, MP [1 ]
Esbenshade, TA [1 ]
Hancock, AA [1 ]
Cowart, MD [1 ]
机构
[1] Abbott Labs, Neurosci Res, Global Pharmaceut Res & Dev, Abbott Pk, IL 60064 USA
关键词
histamine; H3; arylbenzofuran;
D O I
10.1016/j.bmcl.2005.03.047
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
An SAR study of histamine H-3 receptor antagonists based on substituted (R)-2-methyl-1-[2-(5-phenyl-benzofuran-2-yl)ethyl] -pyrrolidines is presented. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2559 / 2563
页数:5
相关论文
共 23 条
[1]   Design, synthesis, and structure-activity relationships of acetylene-based histamine H3 receptor antagonists [J].
Ali, SM ;
Tedford, CE ;
Gregory, R ;
Handley, MK ;
Yates, SL ;
Hirth, WW ;
Phillips, JG .
JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (05) :903-909
[2]   AUTO-INHIBITION OF BRAIN HISTAMINE-RELEASE MEDIATED BY A NOVEL CLASS (H-3) OF HISTAMINE-RECEPTOR [J].
ARRANG, JM ;
GARBARG, M ;
SCHWARTZ, JC .
NATURE, 1983, 302 (5911) :832-837
[3]   Identification of a dual histamine H1/H3 receptor ligand based on the H1 antagonist chlorpheniramine [J].
Aslanian, R ;
Mutahi, MW ;
Shih, NY ;
Piwinski, JJ ;
West, R ;
Williams, SM ;
She, S ;
Wu, RL ;
Hey, JA .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2003, 13 (12) :1959-1961
[4]   Non-imidazole heterocyclic histamine H3 receptor antagonists [J].
Chai, WY ;
Breitenbucher, JG ;
Kwok, A ;
Li, XB ;
Wong, V ;
Carruthers, NI ;
Lovenberg, TW ;
Mazur, C ;
Wilson, SJ ;
Axe, FU ;
Jones, TK .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2003, 13 (10) :1767-1770
[5]   4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention [J].
Cowart, M ;
Faghih, R ;
Curtis, MP ;
Gfesser, GA ;
Bennani, YL ;
Black, LA ;
Pan, LP ;
Marsh, KC ;
Sullivan, JP ;
Esbenshade, TA ;
Fox, GB ;
Hancock, AA .
JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48 (01) :38-55
[6]   Medicinal chemistry and biological properties of non-imidazole histamine H3 antagonists [J].
Cowart, M ;
Altenbach, R ;
Black, L ;
Faghih, R ;
Zhao, C ;
Hancock, AA .
MINI-REVIEWS IN MEDICINAL CHEMISTRY, 2004, 4 (09) :979-992
[7]   A new class of potent non-imidazole H3 antagonists:: 2-aminoethylbenzofurans [J].
Cowart, M ;
Pratt, JK ;
Stewart, AO ;
Bennani, YL ;
Esbenshade, TA ;
Hancock, AA .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2004, 14 (03) :689-693
[8]   AN EFFICIENT AND SELECTIVE METHOD FOR THE PREPARATION OF IODOPHENOLS [J].
EDGAR, KJ ;
FALLING, SN .
JOURNAL OF ORGANIC CHEMISTRY, 1990, 55 (18) :5287-5291
[9]  
ESBENSHADE TA, 2005, J PHARMACOL EXP THER, V313, P615
[10]   Pharmacological properties of ABT-239[4-(2-{2-[(2R)-2-methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]:: II.: Neurophysiological characterization and broad preclinical efficacy in cognition and schizophrenia of a potent and selective histamine H3 receptor antagonist [J].
Fox, GB ;
Esbenshade, TA ;
Pan, JB ;
Radek, RJ ;
Krueger, KM ;
Yao, BB ;
Browman, KE ;
Buckley, MJ ;
Ballard, ME ;
Komater, VA ;
Miner, H ;
Zhang, M ;
Faghih, R ;
Rueter, LE ;
Bitner, RS ;
Drescher, KU ;
Wetter, J ;
Marsh, K ;
Lemaire, M ;
Porsolt, RD ;
Bennani, YL .
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2005, 313 (01) :176-190