Synthesis and SAR of highly potent and selective dopamine D3-receptor antagonists:: 1H-Pyrimidin-2-one derivatives

被引：15

作者：

Geneste, H ^{[1
]}

Backfisch, G

Braje, W

Delzer, J

Haupt, A

Hutchins, CW

King, LL

Kling, A

Teschendorf, HR

Unger, L

Wernet, W

机构：

[1] Abbott GMBH & Co KG, Discovery Res, D-67008 Ludwigshafen, Germany

[2] Abbott GMBH & Co KG, DMPK, D-67008 Ludwigshafen, Germany

[3] Abbott Labs, Adv Technol, Abbott Pk, IL 60064 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 03期

关键词：

dopamine D-3 receptor antagonists; atypical antipsychotics; 1H-pyrimidin-2-ones;

D O I：

10.1016/j.bmcl.2005.10.068

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and SAR of novel highly potent and selective dopamine D-3-receptor antagonists based on a 1H-pyrimidin-2-one scaffold are described. A-690344 antagonized PD 128907-induced huddling deficits in rat (ED50 6.1 mg/kg po), a social interaction paradigm. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：490 / 494

页数：5

共 25 条

[1]

Andriamialisoa Z, 2002, HELV CHIM ACTA, V85, P2926, DOI 10.1002/1522-2675(200209)85:9<2926::AID-HLCA2926>3.0.CO

[2]

2-5

[3]

ARTURSSON P, 1991, CRIT REV THER DRUG, V8, P305

[4]

Ashby CR, 2000, J PHARMACOL EXP THER, V294, P1166

[5] SYNTHESIS OF SOME 5-TRIFLUOROMETHYLPYRIMIDINES [J].

BENNECHE, T ;

UNDHEIM, K .

ACTA CHEMICA SCANDINAVICA SERIES B-ORGANIC CHEMISTRY AND BIOCHEMISTRY, 1984, 38 (06) :505-508

[6] PYRIMIDINE REACTIONS .16. THERMAL REARRANGEMENT OF SUBSTITUTED 2- AND 4-ALKOXYPYRIMIDINES [J].

BROWN, DJ ;

LEE, TC .

AUSTRALIAN JOURNAL OF CHEMISTRY, 1968, 21 (01) :243-&

[7]

DRESCHER K, 2002, 32 ANN M SOC NEUR OR

[8] Fast calculation of molecular polar surface area as a sum of fragment-based contributions and its application to the prediction of drug transport properties [J].

Ertl, P ;

Rohde, B ;

Selzer, P .

JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (20) :3714-3717

[9] SYNTHESIS AND PHOTOCHEMICAL CLEAVAGE OF CIS-SYN PYRIMIDINE CYCLOBUTANE DIMER ANALOGS [J].

FENICK, DJ ;

CARR, HS ;

FALVEY, DE .

JOURNAL OF ORGANIC CHEMISTRY, 1995, 60 (03) :624-631

[10]

GENESTE H, IN PRESS BIOORG MED

← 1 2 3 →