2,4(5)-Diarylimidazoles:: Synthesis and biological evaluation of a new class of sodium channel blockers against hNav1.2

被引：24

作者：

Rivara, Mirko ^{[1
]}

Baheti, Aparna R. ^{[2
]}

Fantini, Marco ^{[1
]}

Cocconcelli, Giuseppe ^{[3
]}

Ghiron, Chiara ^{[3
]}

Kalmar, Christopher L. ^{[2
]}

Singh, Natasha ^{[2
]}

Merrick, Ellen C. ^{[2
]}

Patel, Manoj K. ^{[2
]}

Zuliani, Valentina ^{[1
]}

机构：

[1] Univ Parma, Dipartimento Farmaceut, I-43100 Parma, Italy

[2] Univ Virginia, Dept Anesthesiol, Charlottesville, VA 22908 USA

[3] Siena Biotech SpA, I-53100 Siena, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 20期

关键词：

sodium channel; diarylimidazoles; parallel synthesis;

D O I：

10.1016/j.bmcl.2008.09.036

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A small family of novel 2,4(5)-diarylimidazoles were prepared through a simple and efficient synthesis and evaluated as potential inhibitors of hNa(v)1.2 sodium channel currents. One member of this series (4) exhibited profound inhibition of Na(v)1.2 currents, emerging as a promising lead compound for further structure-activity relationship studies for the development of novel sodium channel blockers. (c) 2008 Elsevier Ltd. All rights reserved.

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页码：5460 / 5462

页数：3

相关论文

共 10 条

[1] CIMETIDINE - NON-THIOUREA H2-RECEPTOR ANTAGONIST [J].

BRIMBLECOMBE, RW ;

DUNCAN, WAM ;

DURANT, GJ ;

EMMETT, JC ;

GANELLIN, CR ;

PARSONS, ME .

JOURNAL OF INTERNATIONAL MEDICAL RESEARCH, 1975, 3 (02) :86-92

[2] Do we need any more new antiepileptic drugs? [J].

Brodie, MJ .

EPILEPSY RESEARCH, 2001, 45 (1-3) :3-6

[3] ANTI-MYCOTIC IMIDAZOLES .4. SYNTHESIS AND ANTIFUNGAL ACTIVITY OF KETOCONAZOLE, A NEW POTENT ORALLY ACTIVE BROAD-SPECTRUM ANTIFUNGAL AGENT [J].

HEERES, J ;

BACKX, LJJ ;

MOSTMANS, JH ;

VANCUTSEM, J .

JOURNAL OF MEDICINAL CHEMISTRY, 1979, 22 (08) :1003-1005

[4] SELECTIVE ANTAGONISTS OF BENZODIAZEPINES [J].

HUNKELER, W ;

MOHLER, H ;

PIERI, L ;

POLC, P ;

BONETTI, EP ;

CUMIN, R ;

SCHAFFNER, R ;

HAEFELY, W .

NATURE, 1981, 290 (5806) :514-516

[5] 2-alkyl-4-arylimidazoles: structurally novel sodium channel modulators [J].

Liberatore, AM ;

Schulz, J ;

Pommier, J ;

Barthelemy, MA ;

Huchet, M ;

Chabrier, PE ;

Bigg, D .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2004, 14 (13) :3521-3523

[6] Butyl 2-(4-[1.1'-biphenyl]-4-yl-1H-imidazol-2-yl)ethylearbamate, a potent sodium channel blocker for the treatment of neuropathic pain [J].

Liberatore, Anne-Marie ;

Schulz, Jocelyne ;

Favre-Guilmard, Christine ;

Pommier, Jacques ;

Lannoy, Jacques ;

Pawlowski, Emilia ;

Barthelemy, Marie-Anne ;

Huchet, Marion ;

Auguet, Michel ;

Chabrier, Pierre-Etienne ;

Bigg, Dennis .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (06) :1746-1749

[7] Molecular and cellular mechanisms of pharmacoresistance in epilepsy [J].

Remy, S ;

Beck, H .

BRAIN, 2006, 129 :18-35

[8] CYP2C19 genotype-related efficacy of omeprazole for the treatment of infection caused by Helicobacter pylori [J].

Tanigawara, Y ;

Aoyama, N ;

Kita, T ;

Shirakawa, K ;

Komada, F ;

Kasuga, M ;

Okumura, K .

CLINICAL PHARMACOLOGY & THERAPEUTICS, 1999, 66 (05) :528-534

[9] ELECTROENCEPHALOGRAPHIC STUDY OF SHORT-ACTING HYPNOTICS ETOMIDATE AND METHOHEXITAL IN DOGS [J].

WAUQUIER, A ;

VANDENBROECK, WAE ;

VERHEYEN, JL ;

JANSSEN, PAJ .

EUROPEAN JOURNAL OF PHARMACOLOGY, 1978, 47 (04) :367-377

[10] A practical synthesis of 2,4(5)-diarylimidazoles from simple building blocks [J].

Zuliani, Valentina ;

Cocconcelli, Giuseppe ;

Fantini, Marco ;

Ghiron, Chiara ;

Rivara, Mirko .

JOURNAL OF ORGANIC CHEMISTRY, 2007, 72 (12) :4551-4553