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Literature DB >> 17446071

Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists.

Abstract

Investigation of a series of heterobicyclic compounds with essential pharmacophoric features of the metabotropic glutamate receptor 5 (mGluR5) antagonists MPEP and MTEP provided novel structural templates with sub-micromolar affinities at the mGluR5.

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Year: 2007 PMID： 17446071 PMCID： PMC1973162 DOI： 10.1016/j.bmcl.2007.03.066

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

26 in total

Review 1. Novel allosteric antagonists shed light on mglu(5) receptors and CNS disorders.

Authors: W P Spooren; F Gasparini; T E Salt; R Kuhn
Journal: Trends Pharmacol Sci Date: 2001-07 Impact factor: 14.819

2. Reinforcing and locomotor stimulant effects of cocaine are absent in mGluR5 null mutant mice.

Authors: C Chiamulera; M P Epping-Jordan; A Zocchi; C Marcon; C Cottiny; S Tacconi; M Corsi; F Orzi; F Conquet
Journal: Nat Neurosci Date: 2001-09 Impact factor: 24.884

Review 3. Discovery and characterization of non-competitive antagonists of group I metabotropic glutamate receptors.

Authors: F Gasparini; P Floersheim; P J Flor; M Heinrich; W Inderbitzin; D Ott; A Pagano; C Stierlin; N Stoehr; I Vranesic; R Kuhn
Journal: Farmaco Date: 2001 Jan-Feb

4. The non-competitive antagonists 2-methyl-6-(phenylethynyl)pyridine and 7-hydroxyiminocyclopropan[b]chromen-1a-carboxylic acid ethyl ester interact with overlapping binding pockets in the transmembrane region of group I metabotropic glutamate receptors.

Authors: A Pagano; D Ruegg; S Litschig; N Stoehr; C Stierlin; M Heinrich; P Floersheim; L Prezèau; F Carroll; J P Pin; A Cambria; I Vranesic; P J Flor; F Gasparini; R Kuhn
Journal: J Biol Chem Date: 2000-10-27 Impact factor: 5.157

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

Authors: Nicholas D P Cosford; Lida Tehrani; Jeffrey Roppe; Edwin Schweiger; Nicholas D Smith; Jeffrey Anderson; Linda Bristow; Jesse Brodkin; Xiaohui Jiang; Ian McDonald; Sara Rao; Mark Washburn; Mark A Varney
Journal: J Med Chem Date: 2003-01-16 Impact factor: 7.446

6. Design and synthesis of novel heterobiaryl amides as metabotropic glutamate receptor subtype 5 antagonists.

Authors: Santosh S Kulkarni; Amy Hauck Newman
Journal: Bioorg Med Chem Lett Date: 2007-01-04 Impact factor: 2.823

7. The mGluR5 antagonist MPEP decreased nicotine self-administration in rats and mice.

Authors: Neil E Paterson; Svetlana Semenova; Fabrizio Gasparini; Athina Markou
Journal: Psychopharmacology (Berl) Date: 2003-04-08 Impact factor: 4.530

8. Antitumor benzothiazoles. 14. Synthesis and in vitro biological properties of fluorinated 2-(4-aminophenyl)benzothiazoles.

Authors: I Hutchinson; M S Chua; H L Browne; V Trapani; T D Bradshaw; A D Westwell; M F Stevens
Journal: J Med Chem Date: 2001-04-26 Impact factor: 7.446

9. L-homocysteine sulfinic acid and other acidic homocysteine derivatives are potent and selective metabotropic glutamate receptor agonists.

Authors: Qi Shi; Jason E Savage; Sandra J Hufeisen; Laura Rauser; Ewa Grajkowska; Paul Ernsberger; Jarda T Wroblewski; Joseph H Nadeau; Bryan L Roth
Journal: J Pharmacol Exp Ther Date: 2003-04 Impact factor: 4.030

10. Morphine conditioned reward is inhibited by MPEP, the mGluR5 antagonist.

Authors: P Popik; M Wróbel
Journal: Neuropharmacology Date: 2002-12 Impact factor: 5.250

14 in total

1. Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists.

Authors: Santosh S Kulkarni; Mu-Fa Zou; Jianjing Cao; Jeffrey R Deschamps; Alice L Rodriguez; P Jeffrey Conn; Amy Hauck Newman
Journal: J Med Chem Date: 2009-06-11 Impact factor: 7.446

2. Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS.

Authors: Ya Zhou; Alice L Rodriguez; Richard Williams; C David Weaver; P Jeffrey Conn; Craig W Lindsley
Journal: Bioorg Med Chem Lett Date: 2009-10-28 Impact factor: 2.823

3. Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5.

Authors: Peng Zhang; Mu-Fa Zou; Alice L Rodriguez; P Jeffrey Conn; Amy Hauck Newman
Journal: Bioorg Med Chem Date: 2010-03-27 Impact factor: 3.641

4. Recent advances in the design and development of novel negative allosteric modulators of mGlu(5).

Authors: Kyle A Emmitte
Journal: ACS Chem Neurosci Date: 2011-08-17 Impact factor: 4.418

5. (3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu(5): Discovery of a new tool compound with activity in the OSS mouse model of addiction.

Authors: Craig W Lindsley; Brittney S Bates; Usha N Menon; Satyawan B Jadhav; Alexander S Kane; Carrie K Jones; Alice L Rodriguez; P Jeffrey Conn; Christopher M Olsen; Danny G Winder; Kyle A Emmitte
Journal: ACS Chem Neurosci Date: 2011-08-17 Impact factor: 4.418

10. A novel and expedient approach to new thiazoles, thiazolo[3,2-a]pyridines, dihydrothiophenes, and hydrazones incorporating thieno[2,3-b]thiophene moiety.

Authors: Yahia Nasser Mabkhot; Assem Barakat; Abdullah Mohammad Al-Majid; Abdullah Saleh Alamary; Taleb T Al-Nahary
Journal: Int J Mol Sci Date: 2012-04-23 Impact factor: 6.208