Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives

Roger J Gillespie; Ian A Cliffe; Claire E Dawson; Colin T Dourish; Suneel Gaur; Paul R Giles; Allan M Jordan; Antony R Knight; Anthony Lawrence; Joanne Lerpiniere; Anil Misra; Robert M Pratt; Richard S Todd; Rebecca Upton; Scott M Weiss; Douglas S Williamson

doi:10.1016/j.bmcl.2008.03.076

Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives

Roger J Gillespie, Ian A Cliffe, Claire E Dawson, Colin T Dourish, Suneel Gaur, Paul R Giles, Allan M Jordan, Antony R Knight, Anthony Lawrence, Joanne Lerpiniere, Anil Misra, Robert M Pratt, Richard S Todd, Rebecca Upton, Scott M Weiss, Douglas S Williamson

Cancer Research UK Manchester Institute

Research output: Contribution to journal › Article › peer-review

Abstract

We describe herein the discovery and development of a series of 4-arylthieno[3,2-d]pyrimidines which are potent adenosine A(2A) receptor antagonists. These novel compounds show high degrees of selectivity against the human A(1), A(2B) and A(3) receptor sub-types. Moreover, a number of these compounds show promising activity in vivo, suggesting potential utility in the treatment of Parkinson's disease.

Original language	English
Pages (from-to)	2920-3
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	9
DOIs	https://doi.org/10.1016/j.bmcl.2008.03.076
Publication status	Published - 1 May 2008

Keywords

Adenosine A1 Receptor Antagonists
Adenosine A2 Receptor Antagonists
Adenosine A3 Receptor Antagonists
Antiparkinson Agents
Drug Design
Humans
Models, Chemical
Parkinsonian Disorders
Pyrimidines
Stereoisomerism
Structure-Activity Relationship

Research Beacons, Institutes and Platforms

Manchester Cancer Research Centre

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.bmcl.2008.03.076

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Gillespie, R. J., Cliffe, I. A., Dawson, C. E., Dourish, C. T., Gaur, S., Giles, P. R., Jordan, A. M., Knight, A. R., Lawrence, A., Lerpiniere, J., Misra, A., Pratt, R. M., Todd, R. S., Upton, R., Weiss, S. M., & Williamson, D. S. (2008). Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives. Bioorganic and Medicinal Chemistry Letters, 18(9), 2920-3. https://doi.org/10.1016/j.bmcl.2008.03.076

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title = "Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives",

abstract = "We describe herein the discovery and development of a series of 4-arylthieno[3,2-d]pyrimidines which are potent adenosine A(2A) receptor antagonists. These novel compounds show high degrees of selectivity against the human A(1), A(2B) and A(3) receptor sub-types. Moreover, a number of these compounds show promising activity in vivo, suggesting potential utility in the treatment of Parkinson's disease.",

keywords = "Adenosine A1 Receptor Antagonists, Adenosine A2 Receptor Antagonists, Adenosine A3 Receptor Antagonists, Antiparkinson Agents, Drug Design, Humans, Models, Chemical, Parkinsonian Disorders, Pyrimidines, Stereoisomerism, Structure-Activity Relationship",

author = "Gillespie, {Roger J} and Cliffe, {Ian A} and Dawson, {Claire E} and Dourish, {Colin T} and Suneel Gaur and Giles, {Paul R} and Jordan, {Allan M} and Knight, {Antony R} and Anthony Lawrence and Joanne Lerpiniere and Anil Misra and Pratt, {Robert M} and Todd, {Richard S} and Rebecca Upton and Weiss, {Scott M} and Williamson, {Douglas S}",

year = "2008",

month = may,

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doi = "10.1016/j.bmcl.2008.03.076",

language = "English",

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pages = "2920--3",

journal = "Bioorganic and Medicinal Chemistry Letters",

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Gillespie, RJ, Cliffe, IA, Dawson, CE, Dourish, CT, Gaur, S, Giles, PR, Jordan, AM, Knight, AR, Lawrence, A, Lerpiniere, J, Misra, A, Pratt, RM, Todd, RS, Upton, R, Weiss, SM & Williamson, DS 2008, 'Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives', Bioorganic and Medicinal Chemistry Letters, vol. 18, no. 9, pp. 2920-3. https://doi.org/10.1016/j.bmcl.2008.03.076

TY - JOUR

T1 - Antagonists of the human adenosine A2A receptor. Part 2

T2 - Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives

AU - Gillespie, Roger J

AU - Cliffe, Ian A

AU - Dawson, Claire E

AU - Dourish, Colin T

AU - Gaur, Suneel

AU - Giles, Paul R

AU - Jordan, Allan M

AU - Knight, Antony R

AU - Lawrence, Anthony

AU - Lerpiniere, Joanne

AU - Misra, Anil

AU - Pratt, Robert M

AU - Todd, Richard S

AU - Upton, Rebecca

AU - Weiss, Scott M

AU - Williamson, Douglas S

PY - 2008/5/1

Y1 - 2008/5/1

N2 - We describe herein the discovery and development of a series of 4-arylthieno[3,2-d]pyrimidines which are potent adenosine A(2A) receptor antagonists. These novel compounds show high degrees of selectivity against the human A(1), A(2B) and A(3) receptor sub-types. Moreover, a number of these compounds show promising activity in vivo, suggesting potential utility in the treatment of Parkinson's disease.

AB - We describe herein the discovery and development of a series of 4-arylthieno[3,2-d]pyrimidines which are potent adenosine A(2A) receptor antagonists. These novel compounds show high degrees of selectivity against the human A(1), A(2B) and A(3) receptor sub-types. Moreover, a number of these compounds show promising activity in vivo, suggesting potential utility in the treatment of Parkinson's disease.

KW - Adenosine A1 Receptor Antagonists

KW - Adenosine A2 Receptor Antagonists

KW - Adenosine A3 Receptor Antagonists

KW - Antiparkinson Agents

KW - Drug Design

KW - Humans

KW - Models, Chemical

KW - Parkinsonian Disorders

KW - Pyrimidines

KW - Stereoisomerism

KW - Structure-Activity Relationship

U2 - 10.1016/j.bmcl.2008.03.076

DO - 10.1016/j.bmcl.2008.03.076

M3 - Article

C2 - 18407496

SN - 1464-3405

VL - 18

SP - 2920

EP - 2923

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 9

ER -

Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives

Abstract

Keywords

Research Beacons, Institutes and Platforms

UN SDGs

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