Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpurines

Roger J Gillespie; Ian A Cliffe; Claire E Dawson; Colin T Dourish; Suneel Gaur; Allan M Jordan; Antony R Knight; Joanne Lerpiniere; Anil Misra; Robert M Pratt; Jonathan Roffey; Gemma C Stratton; Rebecca Upton; Scott M Weiss; Douglas S Williamson

doi:10.1016/j.bmcl.2008.03.072

Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpurines

Roger J Gillespie
, Ian A Cliffe
, Claire E Dawson
, Colin T Dourish
, Suneel Gaur
, Allan M Jordan
, Antony R Knight
, Joanne Lerpiniere
, Anil Misra
, Robert M Pratt
, Jonathan Roffey
, Gemma C Stratton
, Rebecca Upton
, Scott M Weiss
, Douglas S Williamson

Cancer Research UK Manchester Institute

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

Abstract

A series of pyrazolo[3,4-d]pyrimidine, pyrrolo[2,3-d]pyrimidine and 6-arylpurine adenosine A(2A) antagonists is described. Many examples were highly selective against the human A(1) receptor sub-type and were active in an in vivo model of Parkinson's disease.

Original language	English
Pages (from-to)	2924-9
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	9
DOIs	https://doi.org/10.1016/j.bmcl.2008.03.072
Publication status	Published - 1 May 2008

Keywords

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

Research Beacons, Institutes and Platforms

Manchester Cancer Research Centre

Access to Document

10.1016/j.bmcl.2008.03.072

Cite this

Gillespie, R. J., Cliffe, I. A., Dawson, C. E., Dourish, C. T., Gaur, S., Jordan, A. M., Knight, A. R., Lerpiniere, J., Misra, A., Pratt, R. M., Roffey, J., Stratton, G. C., Upton, R., Weiss, S. M., & Williamson, D. S. (2008). Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpurines. Bioorganic and Medicinal Chemistry Letters, 18(9), 2924-9. https://doi.org/10.1016/j.bmcl.2008.03.072

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title = "Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpurines",

abstract = "A series of pyrazolo[3,4-d]pyrimidine, pyrrolo[2,3-d]pyrimidine and 6-arylpurine adenosine A(2A) antagonists is described. Many examples were highly selective against the human A(1) receptor sub-type and were active in an in vivo model of Parkinson's disease.",

keywords = "Adenosine A1 Receptor Antagonists, Adenosine A2 Receptor Antagonists, Antiparkinson Agents, Drug Design, Humans, Models, Chemical, Parkinsonian Disorders, Purines, Pyrazoles, 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 Jordan, \{Allan M\} and Knight, \{Antony R\} and Joanne Lerpiniere and Anil Misra and Pratt, \{Robert M\} and Jonathan Roffey and Stratton, \{Gemma C\} and Rebecca Upton and Weiss, \{Scott M\} and Williamson, \{Douglas S\}",

year = "2008",

month = may,

day = "1",

doi = "10.1016/j.bmcl.2008.03.072",

language = "English",

volume = "18",

pages = "2924--9",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "1464-3405",

publisher = "Elsevier BV",

number = "9",

}

Gillespie, RJ, Cliffe, IA, Dawson, CE, Dourish, CT, Gaur, S, Jordan, AM, Knight, AR, Lerpiniere, J, Misra, A, Pratt, RM, Roffey, J, Stratton, GC, Upton, R, Weiss, SM & Williamson, DS 2008, 'Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpurines', Bioorganic and Medicinal Chemistry Letters, vol. 18, no. 9, pp. 2924-9. https://doi.org/10.1016/j.bmcl.2008.03.072

TY - JOUR

T1 - Antagonists of the human adenosine A2A receptor. Part 3

T2 - Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpurines

AU - Gillespie, Roger J

AU - Cliffe, Ian A

AU - Dawson, Claire E

AU - Dourish, Colin T

AU - Gaur, Suneel

AU - Jordan, Allan M

AU - Knight, Antony R

AU - Lerpiniere, Joanne

AU - Misra, Anil

AU - Pratt, Robert M

AU - Roffey, Jonathan

AU - Stratton, Gemma C

AU - Upton, Rebecca

AU - Weiss, Scott M

AU - Williamson, Douglas S

PY - 2008/5/1

Y1 - 2008/5/1

N2 - A series of pyrazolo[3,4-d]pyrimidine, pyrrolo[2,3-d]pyrimidine and 6-arylpurine adenosine A(2A) antagonists is described. Many examples were highly selective against the human A(1) receptor sub-type and were active in an in vivo model of Parkinson's disease.

AB - A series of pyrazolo[3,4-d]pyrimidine, pyrrolo[2,3-d]pyrimidine and 6-arylpurine adenosine A(2A) antagonists is described. Many examples were highly selective against the human A(1) receptor sub-type and were active in an in vivo model of Parkinson's disease.

KW - Adenosine A1 Receptor Antagonists

KW - Adenosine A2 Receptor Antagonists

KW - Antiparkinson Agents

KW - Drug Design

KW - Humans

KW - Models, Chemical

KW - Parkinsonian Disorders

KW - Purines

KW - Pyrazoles

KW - Pyrimidines

KW - Stereoisomerism

KW - Structure-Activity Relationship

U2 - 10.1016/j.bmcl.2008.03.072

DO - 10.1016/j.bmcl.2008.03.072

M3 - Article

C2 - 18411049

SN - 1464-3405

VL - 18

SP - 2924

EP - 2929

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 9

ER -

Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpurines

Abstract

Keywords

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