A new series of pyridinyl-alkynes as antagonists of the metabotropic glutamate receptor 5 (mGluR5)

被引：19

作者：

Bach, Peter

Nilsson, Karolina

Wallberg, Andreas

Bauer, Udo

Hammerland, Lance G.

Peterson, Alecia

Svensson, Tor

Osterlund, Krister

Karis, David

Boije, Maria

Wensbo, David

机构：

[1] AstraZeneca R&D, Dept Med Chem, S-43183 Molndal, Sweden

[2] NPS Pharmaceut, Salt Lake City, UT 84108 USA

[3] AstraZeneca R&D Sodertalje, Dept Med Chem, Local Discovery CNS & Pain Control, S-15185 Sodertalje, Sweden

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 18期

关键词：

mGluR5; antagonists; pyridinyl-alkynes; propargyl ethers; SAR;

D O I：

10.1016/j.bmcl.2006.06.079

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

引用

页码：4792 / 4795

页数：4

共 26 条

[1]

ABE T, 1992, J BIOL CHEM, V267, P13361

[2] Synthesis and receptor assay of aromatic-ethynyl-aromatic derivatives with potent mGluR5 antagonist activity [J].

Alagille, D ;

Baldwin, RM ;

Roth, BL ;

Wroblewski, JT ;

Grajkowska, E ;

Tamagnan, GD .

BIOORGANIC & MEDICINAL CHEMISTRY, 2005, 13 (01) :197-209

[3]

BACH P, Patent No. 2005044265

[4] G-protein coupled receptors: Models, mutagenesis, and drug design [J].

Bikker, JA ;

Trumpp-Kallmeyer, S ;

Humblet, C .

JOURNAL OF MEDICINAL CHEMISTRY, 1998, 41 (16) :2911-2927

[5] Anxiolytic-like activity of the mGluR5 antagonist MPEP - A comparison with diazepam and buspirone [J].

Brodkin, J ;

Busse, C ;

Sukoff, SJ ;

Varney, MA .

PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR, 2002, 73 (02) :359-366

[6] Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists [J].

Chua, PC ;

Nagasawa, JY ;

Bleicher, LS ;

Munoz, B ;

Schweiger, EJ ;

Tehrani, L ;

Anderson, JJ ;

Cramer, M ;

Chung, J ;

Green, MD ;

King, CD ;

Reyes-Manalo, G ;

Cosford, NDP .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (20) :4589-4593

[7] 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: A potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity [J].

Cosford, NDP ;

Tehrani, L ;

Roppe, J ;

Schweiger, E ;

Smith, ND ;

Anderson, J ;

Bristow, L ;

Brodkin, J ;

Jiang, XH ;

McDonald, I ;

Rao, S ;

Washburn, M ;

Varney, MA .

JOURNAL OF MEDICINAL CHEMISTRY, 2003, 46 (02) :204-206

[8] [3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy:: Potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor [J].

Cosford, NDP ;

Roppe, J ;

Tehrani, L ;

Schweiger, EJ ;

Seiders, TJ ;

Chaudary, A ;

Rao, S ;

Varney, MA .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2003, 13 (03) :351-354

[9] METHOXYTETRAHYDROPYRANS - A NEW SERIES OF SELECTIVE AND ORALLY POTENT 5-LIPOXYGENASE INHIBITORS [J].

CRAWLEY, GC ;

DOWELL, RI ;

EDWARDS, PN ;

FOSTER, SJ ;

MCMILLAN, RM ;

WALKER, ERH ;

WATERSON, D ;

BIRD, TGC ;

BRUNEAU, P ;

GIRODEAU, JM .

JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (14) :2600-2609

[10]

CRAWLY GC, Patent No. 1990385680

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