5-Cyclic Amine-3-arylsulfonylindazoles as Novel 5-HT6 Receptor Antagonists

被引：20

作者：

Haydar, Simon N. ^{[1
]}

Yun, Heedong ^{[1
]}

Andrae, Patrick M. ^{[1
]}

Mattes, James ^{[1
]}

Zhang, Jean ^{[2
]}

Kramer, Angela ^{[2
]}

Smith, Deborah L. ^{[2
]}

Huselton, Christine ^{[3
]}

Graf, Radka ^{[2
]}

Aschmies, Suzan ^{[2
]}

Schechter, Lee E. ^{[2
]}

Comery, Thomas A. ^{[2
]}

Robichaud, Albert J. ^{[1
]}

机构：

[1] Wyeth Ayerst Res, Chem Sci, Princeton, NJ 08543 USA

[2] Wyeth Ayerst Res, Discovery Neurosci, Princeton, NJ 08543 USA

[3] Wyeth Ayerst Res, Drug Safety & Metab, Collegeville, PA 19426 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 53卷 / 06期

关键词：

ACETYLCHOLINE-RELEASE; POTENT; DERIVATIVES; LOCALIZATION; DISCOVERY; SB-271046; HYDROGEN; LIGANDS; CORTEX;

D O I：

10.1021/jm901674f

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel 5-cyclic amine-3-arylsulfonylindazoles were prepared, and several analogues within this class have been identified as high-affinity 5-HT6 receptor ligands with improved pharmacokinetic and pharmacological properties. One selected example, 18b, showed good brain penetrability and a generally favorable pharmacokinetic profile with procognitive efficacy in the rat novel object recognition assay. The synthesis and structure activity relationship of this potent class are discussed.

引用

页码：2521 / 2527

页数：7

共 50 条

[41] 5-HT6 receptor antagonists as treatment for age-related cognitive decline
Quiedeville, Anne
Boulouard, Michel
Costa-Aze, Virginie Da Silva
Dauphin, Francois
Bouet, Valentine
Freret, Thomas
REVIEWS IN THE NEUROSCIENCES, 2014, 25 (03) : 417 - 427
[42] Effect of two 5-HT6 receptor antagonists on the rat liver: a molecular approach
L Suter
M Haiker
M C de Vera
S Albertini
The Pharmacogenomics Journal, 2003, 3 : 320 - 334
[43] 5-HT6 receptor antagonists enhance retention of a water maze task in the rat
Rogers, DC
Hagan, JJ
PSYCHOPHARMACOLOGY, 2001, 158 (02) : 114 - 119
[44] Tricyclic azepine derivatives as selective brain penetrant 5-HT6 receptor antagonists
Trani, Giancarlo
Baddeley, Stuart M.
Briggs, Michael A.
Chuang, Tsu T.
Deeks, Nigel J.
Johnson, Christopher N.
Khazragi, Abir A.
Mead, Tania L.
Medhurst, Andrew D.
Milner, Peter H.
Quinn, Leann P.
Ray, Alison M.
Rivers, Dean A.
Stean, Tania O.
Stemp, Geoffrey
Trail, Brenda K.
Witty, David R.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (20) : 5698 - 5700
[45] Serotonergic 5-HT6 Receptor Antagonists: Heterocyclic Chemistry and Potential Therapeutic Significance
Bali, Alka
Singh, Shalu
CURRENT TOPICS IN MEDICINAL CHEMISTRY, 2015, 15 (17) : 1643 - 1662
[46] 5-HT6 Receptor Antagonists: Potential Efficacy for the Treatment of Cognitive Impairment in Schizophrenia
de Bruin, Natasja M. W. J.
Kruse, Chris G.
CURRENT PHARMACEUTICAL DESIGN, 2015, 21 (26) : 3739 - 3759
[47] 5-HT6 receptor antagonists enhance retention of a water maze task in the rat
Rogers D.C.
Hagan J.J.
Psychopharmacology, 2001, 158 (2) : 114 - 119
[48] 5-HT6 receptor antagonists:: Prospects for the treatment of cognitive disorders including dementia
Johnson, Christopher N.
Ahmed, Mahmood
Miller, Neil D.
CURRENT OPINION IN DRUG DISCOVERY & DEVELOPMENT, 2008, 11 (05) : 642 - 654
[49] 5-HT6 receptor antagonists improve performance in an attentional set shifting task
Hatcher, PD
Brown, VJ
Tait, DS
Jones, DNC
JOURNAL OF PSYCHOPHARMACOLOGY, 2002, 16 (03) : A16 - A16
[50] Effect of two 5-HT6 receptor antagonists on the rat liver:: a molecular approach
Suter, L
Haiker, M
de Vera, MC
Albertini, S
PHARMACOGENOMICS JOURNAL, 2003, 3 (06): : 320 - 334

← 1 2 3 4 5 →