Výsledky vyhledávání - "Barry Peter Clark"

Synthesis and Pharmacological Characterization of C4-Disubstituted Analogs of 1S,2S,5R,6S-2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylate: Identification of a Potent, Selective Metabotropic Glutamate Receptor Agonist and Determination of Agonist-Bound Human mGlu2 and mGlu3 Amino Terminal Domain Structures

Publikováno v: Journal of Medicinal Chemistry. 58:1776-1794

As part of our ongoing research to identify novel agents acting at metabotropic glutamate 2 (mGlu2) and 3 (mGlu3) receptors, we have previously reported the identification of the C4α-methyl analog of mGlu2/3 receptor agonist 1 (LY354740). This molec

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::527bce29ceb86979086e1027b9d87633
https://doi.org/10.1021/jm501612y

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Discovery of (1R,2R)-N-(4-(6-isopropylpyridin-2-yl)-3-(2-methyl-2H-indazol-5-yl)isothiazol-5-yl)-2-methylcyclopropanecarboxamide, a potent and orally efficacious mGlu5 receptor negative allosteric modulator

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 23:1249-1252

A novel series of selective negative allosteric modulators (NAMs) for metabotropic glutamate receptor 5 (mGlu5) was discovered from an isothiazole scaffold. One compound of this series, (1R,2R)-N-(4-(6-isopropylpyridin-2-yl)-3-(2-methyl-2H-indazol-5-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ef86f59bea2ecb1e4670f9d5e462c59f
https://doi.org/10.1016/j.bmcl.2013.01.009

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Stereoselective Synthesis of β-(Hydroxymethylaryl/alkyl)-α-methylene-γ-butyrolactones

Autor: Barry Peter Clark, Eric P. A. Talbot, David M. Hodgson

Publikováno v: Organic Letters. 13:2594-2597

Zinc or a chromium(II) source with 3-(bromomethyl)furan-2(5H)-one (3) and an aldehyde gives β-(hydroxymethylaryl/alkyl)-α-methylene-γ-butyrolactones 5 in good yields and high diastereoselectivities. The methodology is demonstrated in concise synth

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f42937893a6589f3bfe013512c91bea0
https://doi.org/10.1021/ol200711f

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N-Alkyl-N-arylmethylpiperidin-4-amines: Novel dual inhibitors of serotonin and norepinephrine reuptake

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 16:2714-2718

A series of N-alkyl-N-arylmethylpiperidin-4-amines have been prepared and are demonstrated to be inhibitors of both serotonin and norepinephrine reuptake.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a56cf54d2383026d2ed507a24225e03a
https://doi.org/10.1016/j.bmcl.2006.02.008

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Phenylglycine derivatives as antagonists of group III metabotropic glutamate receptors expressed on neonatal rat primary afferent terminals

Autor: David E. Jane, Barry Peter Clark, Stuart J. Conway, Patrick A Howson, Richard V Williams, Jacqueline C. Miller

Publikováno v: British Journal of Pharmacology. 139:1523-1531

1 Three novel phenylglycine analogues; (RS)-a-methyl-3-chloro-4-phosphonophenylglycine (UBP1110), (RS)-a-methyl-3-methoxy-4-phosphonophenylglycine (UBP1111) and (RS)-a-methyl-3methyl-4-phosphonophenylglycine (UBP1112) antagonised the depression of th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c8f480de2502c877f3b5894fac72d1f4
https://doi.org/10.1038/sj.bjp.0705377

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Inhibition of group I metabotropic glutamate receptor responses in vivo in rats by a new generation of carboxyphenylglycine-like amino acid antagonists

Autor: Bryan G. Johnson, Joseph P. Tizzano, Michael P. Johnson, Kelly I. Griffey, Darryle D. Schoepp, Rebecca A. Wright, John R. Harris, Gerald Kelly, Ann E. Kingston, Mary Jo Chamberlain, Rosemarie Tomlinson, Barry Peter Clark, Richard S. Baker

Publikováno v: Neuroscience Letters. 330:127-130

A series of novel group I metabotropic glutamate receptor (mGlu) antagonists have been designed on the basis of the 4-carboxyphenylglycine pharmacophore. The compounds are either mGlu1 receptor selective or equipotent for both mGlu1 and mGlu5 recepto

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f1cbdd09122fcc04534fbba2a2c6b34a
https://doi.org/10.1016/s0304-3940(02)00751-6

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The role of type 1 metabotropic glutamate receptors in the generation of dorsal root reflexes induced by acute arthritis or the spinal infusion of 4-aminopyridine in the anesthetized rat

Autor: Liping Zhang, Barry Peter Clark, Y. Chen, Emanuele Sher, Karin N. Westlund

Publikováno v: The Journal of Pain. 1:151-161

An erratum was published for this article in the Fall, part 1 issue of The Journal of Pain (Vol 1, No 3, pp 243). Antidromically propagated action potentials can be recorded in the proximal end of the severed medial articular nerve (MAN) on mechanica

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2d9ebabba91ac13dbc96282a86b53532
https://doi.org/10.1016/s1526-5900(00)90100-7

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Evaluation of the activity of a novel metabotropic glutamate receptor antagonist (±)-2-amino-2-(3-cis and trans-carboxycyclobutyl-3-(9-thioxanthyl)propionic acid) in the in vitro neonatal spinal cord and in an in vivo pain model

Autor: G. Bacon, A.E. Kingston, Barry Peter Clark, B.G. Johnson, Y. Chen, Emanuele Sher, Mary Jeanne Kallman, D D Schoepp, Rebecca A. Wright

Publikováno v: Neuroscience. 95:787-793

The cyclobutylglycine (+/-)-2-amino-2-(3-cis and trans-carboxycyclobutyl-3-(9-thioxanthyl)propionic acid) (LY393053) has been identified as a functionally potent metabotropic glutamate receptor antagonist. It is most potent on the two group I metabot

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::37fb1a278a55ab3dc41ee38ab8d3f8eb
https://doi.org/10.1016/s0306-4522(99)00496-0

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Syntheses of 7-Carboxyindolylglycines Utilising Glycine Cation Equivalents

Autor: Barry Peter Clark, John Richard Harris

Publikováno v: Synthetic Communications. 27:4223-4234

Abstract: The synthesis of two 7-carboxyindolylglycines is described as putative metabotropic glutamate receptor (mGluR) antagonists, employing glycine cation equivalents in the key steps.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::30dcc87f45c66a2f8e2f17eff08cc4a6
https://doi.org/10.1080/00397919708005046

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