Výsledky vyhledávání - "and Andrew Thurkauf"

Design, synthesis, and discovery of 5-piperazinyl-1,2,6,7-tetrahydro-5H-azepino[3,2,1-hi]indol-4-one derivatives: A novel series of mixed dopamine D2/D4 receptor antagonist

Autor: Jack Hammer, He Zhao, Charles J. Manly, Robbin Brodbeck, Renee Primus, Andrzej Kieltyka, Andrew Thurkauf, Jayaraman Chandrasekhar, Stanislaw Rachwal, Xiaoyan Zhang, Kevin J. Hodgetts

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 13:701-704

5-piperazinyl-1,2,6,7-tetrahydro-5H-azepino[3,2,1-hi]indol-4-one derivatives were designed, synthesized, and identified as a new series of mixed dopamine D(2)/D(4) receptor antagonists. This series featured a rigid tricyclic ring system as an importa

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d838ce696cd6b9f68c9b403a0901ae31
https://doi.org/10.1016/s0960-894x(02)01056-9

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Indoline and piperazine containing derivatives as a novel class of mixed D2/D4 receptor antagonists. Part 1: Identification and structure–activity relationships

Autor: Hutchison Alan J, Kover Renata X, Robbin Brodbeck, Xiao-Shu He, Andrew Thurkauf, Kevin J. Hodgetts, Andrzej Kieltyka, Stanislaw Rachwal, Xiaoyan Zhang, John R. Peterson, Jan W. F. Wasley, Renee J. Primus, He Zhao

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 12:3105-3109

Optimization of the lead compound 2-[-4-(4-chloro-benzyl)-piperazin-1-yl]-1-(2,3-dihydro-indol-1-yl)-ethanone 1 by systematic structure-activity relation (SAR) studies lead to two potent compounds 2-[-4-(4-chloro-benzyl)-piperazin-1-yl]-1-(2-methy-2,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eb02ce198fbc302c0f8d14590d286292
https://doi.org/10.1016/s0960-894x(02)00655-8

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Indoline and piperazine containing derivatives as a novel class of mixed D2/D4 receptor antagonists. Part 2: Asymmetric synthesis and biological evaluation

Autor: Xiao-Shu He, Andrew Thurkauf, Andrzej Kieltyka, Jan W. F. Wasley, Robbin Brodbeck, He Zhao, Diane C. Hoffman, Renee J. Primus

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 12:3111-3115

A series of chiral benzylpiperazinyl-1-(2,3-dihydro-indol-1-yl)ethanone derivatives were prepared and examined for their affinity at dopamine D2 and D4 receptors. Three compounds having D2/D4 affinity ratios approximating that found for the atypical

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b5e0fd275bd4e4a19ae2bd12af99f435
https://doi.org/10.1016/s0960-894x(02)00656-x

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6-(4-Benzylpiperazin-1-yl)benzodioxanes as selective ligands at cloned primate dopamine D4 receptors

Autor: Jan W. F. Wasley, Kevin J. Hodgetts, Jennifer Tran, Andrew Thurkauf, Robbin Brodbeck, Andrzej Kieltyka

Publikováno v: Bioorganic & Medicinal Chemistry. 9:3207-3213

A series of novel 6-(4-benzylpiperazin-1-yl)benzodioxanes were prepared and screened at selected dopamine receptor subtypes. 6-(4-[4-Chlorobenzyl]piperazin-1-yl)benzodioxane (2d) had high affinity and selectivity for the D(4) dopamine receptor subtyp

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f1ed98e2c5f3546ebaaa185570b3e4e6
https://doi.org/10.1016/s0968-0896(01)00226-7

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Design and Synthesis of [(2,3-Dichlorophenyl)piperazin-1-yl]alkylfluorenylcarboxamides as Novel Ligands Selective for the Dopamine D3Receptor Subtype

Autor: and Andrew Thurkauf, Andrzej Kieltyka, Amy Hauck Newman, Michael J. Robarge, Robbin Brodbeck, Stephen M. Husbands

Publikováno v: Journal of Medicinal Chemistry. 44:3175-3186

The dopamine D3 receptor subtype has been recently targeted as a potential neurochemical modulator of the behavioral actions of psychomotor stimulants, such as cocaine. However, definitive behavioral investigations have been hampered by the lack of h

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e3264fbdc66e4a3e2721ed118cb1fa7f
https://doi.org/10.1021/jm010146o

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A PRACTICAL AND CONVENIENT SYNTHESIS OF METHYL 5-FORMYL-3-METHOXYBENZOATE

Autor: He Zhao, Andrew Thurkauf

Publikováno v: Synthetic Communications. 31:1921-1926

A practical and convenient synthesis of methyl 5-formyl-3-methoxybenzoate starting from 3-hydroxy-5-(methoxycarbonyl)benzoate in 65% overall yield is described. Ethyl 5-formyl-3-methoxybenzoate was also prepared in the similar manner.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::142742071b9699bcabd99418f97d280f
https://doi.org/10.1081/scc-100104344

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trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: Mixed Dopamine D2/D4 Receptor Antagonists as Potential Antipsychotic Agents

Autor: Maria D. Bacolod, Andrew Thurkauf, Xiaoyan Zhang, Andrzej Kieltyka, Jennifer Tran, Jan W. F. Wasley, He Zhao, Robbin Brodbeck, Brian Girard, Kevin J. Hodgetts, Diane C. Hoffman, Kimberly Craven, Stanislaw Rachwal

Publikováno v: Journal of Medicinal Chemistry. 43:3923-3932

The dopaminergic receptor profile of a series of trans-1-[(2-phenylcyclopropyl)methyl]-4-arylpiperazines was examined. Aromatic substitution patterns were varied with the goal of identifying a compound having affinities for the D(2) and D(4) receptor

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::69ebbd3228b62f4930f7bbde7a791a72
https://doi.org/10.1021/jm990562x

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Design, synthesis, and discovery of 3-piperazinyl-3,4-dihydro-2(1H)-quinolinone derivatives

Autor: Andrew Thurkauf, Julia Braun, He Zhao, Andrzej Kieltyka, Robin Brodbeck

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 10:2119-2122

3-Piperazinyl-3,4-dihydro-2(1 H )-quinolinone derivatives (δ-lactams) were designed, synthesized, and identified as a new series of mixed dopamine D 2 /D 4 receptor antagonists. To further the structure–activity relationship (SAR) study, 3-piperaz

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::3063321086755da7b0790cdb44aa33a3
https://doi.org/10.1016/s0960-894x(00)00421-2

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The synthesis of tritiated 2-phenyl-4-[4-(2-pyrimidyl)piperazinyl]methylimidazole ([3H] NGD 94-1), a ligand selective for the dopamine D4 receptor subtype

Autor: Andrew Thurkauf

Publikováno v: Journal of Labelled Compounds and Radiopharmaceuticals. 39:123-128

A tritiated ligand for the dopamine D 4 receptor subtype, 2-phenyl-4-[4-(2-pyrimidyl) piperazinyl] methylimidazole ([ 3 H] NGD 94-1), was prepared in six steps starting with 3, 5-dichlorobenzonitrile. NGD 94-1 was shown to have a greater than 500 fol

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::eee4eab83999247551dd8d4c298dadd4
https://doi.org/10.1002/(sici)1099-1344(199702)39:2<123::aid-jlcr959>3.0.co

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