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Article ; Online: Substituted thieno[2,3-d]pyrimidines as adenosine A2A receptor antagonists.

Shook, Brian C / Chakravarty, Devraj / Barbay, J Kent / Wang, Aihua / Leonard, Kristi / Alford, Vernon / Powell, Mark T / Rassnick, Stefanie / Scannevin, Robert H / Carroll, Karen / Wallace, Nathaniel / Crooke, Jeffrey / Ault, Mark / Lampron, Lisa / Westover, Lori / Rhodes, Kenneth / Jackson, Paul F

Bioorganic & medicinal chemistry letters

2013 Volume 23, Issue 9, Page(s) 2688–2691

Abstract: A novel series of benzyl substituted thieno[2,3-d]pyrimidines were identified as potent A2A receptor antagonists. Several five- and six-membered heterocyclic replacements for the optimized methylfuran were explored. Select compounds effectively reverse ... ...

Abstract	A novel series of benzyl substituted thieno[2,3-d]pyrimidines were identified as potent A2A receptor antagonists. Several five- and six-membered heterocyclic replacements for the optimized methylfuran were explored. Select compounds effectively reverse catalepsy in mice when dosed orally.
MeSH term(s)	Adenosine A2 Receptor Antagonists/chemistry ; Adenosine A2 Receptor Antagonists/pharmacokinetics ; Adenosine A2 Receptor Antagonists/therapeutic use ; Animals ; Brain/metabolism ; Catalepsy/drug therapy ; Half-Life ; Humans ; Kinetics ; Mice ; Protein Binding ; Pyrimidines/chemistry ; Pyrimidines/pharmacokinetics ; Pyrimidines/therapeutic use ; Rats ; Receptor, Adenosine A2A/chemistry ; Receptor, Adenosine A2A/metabolism
Chemical Substances	Adenosine A2 Receptor Antagonists ; Pyrimidines ; Receptor, Adenosine A2A
Language	English
Publishing date	2013-05-01
Publishing country	England
Document type	Journal Article
ZDB-ID	1063195-1
ISSN	1464-3405 ; 0960-894X
ISSN (online)	1464-3405
ISSN	0960-894X
DOI	10.1016/j.bmcl.2013.02.078
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article: Synthesis and SAR of alpha-sulfonylcarboxylic acids as potent matrix metalloproteinase inhibitors.

Zhang, Yue-Mei / Fan, Xiaodong / Xiang, Bangping / Chakravarty, Devraj / Scannevin, Robert / Burke, Sharon / Karnachi, Prabha / Rhodes, Kenneth / Jackson, Paul

Bioorganic & medicinal chemistry letters

2006 Volume 16, Issue 12, Page(s) 3096–3100

Abstract: A series of novel carboxylic acid-based alpha-sulfone MMP inhibitors have been synthesized and the in vitro enzyme SAR is discussed. A potential binding mode in the active site of the MMP-9 homology model was highlighted. These compounds are potent MMP-9 ...

Abstract	A series of novel carboxylic acid-based alpha-sulfone MMP inhibitors have been synthesized and the in vitro enzyme SAR is discussed. A potential binding mode in the active site of the MMP-9 homology model was highlighted. These compounds are potent MMP-9 inhibitors and are selective over MMP-1.
MeSH term(s)	Animals ; Carboxylic Acids/chemical synthesis ; Carboxylic Acids/chemistry ; Carboxylic Acids/pharmacology ; Inhibitory Concentration 50 ; Matrix Metalloproteinase Inhibitors ; Matrix Metalloproteinases/chemistry ; Matrix Metalloproteinases/metabolism ; Models, Molecular ; Molecular Structure ; Protease Inhibitors/chemistry ; Protease Inhibitors/pharmacokinetics ; Protease Inhibitors/pharmacology ; Rats ; Structure-Activity Relationship ; Sulfur/chemistry
Chemical Substances	Carboxylic Acids ; Matrix Metalloproteinase Inhibitors ; Protease Inhibitors ; Sulfur (70FD1KFU70) ; Matrix Metalloproteinases (EC 3.4.24.-)
Language	English
Publishing date	2006-06-15
Publishing country	England
Document type	Journal Article
ZDB-ID	1063195-1
ISSN	1464-3405 ; 0960-894X
ISSN (online)	1464-3405
ISSN	0960-894X
DOI	10.1016/j.bmcl.2006.03.065
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Article: Substituted thieno[2,3-d]pyrimidines as adenosine A₂A receptor antagonists

Shook, Brian C / Chakravarty, Devraj / Barbay, J. Kent / Wang, Aihua / Leonard, Kristi / Alford, Vernon / Powell, Mark T / Rassnick, Stefanie / Scannevin, Robert H / Carroll, Karen / Wallace, Nathaniel / Crooke, Jeffrey / Ault, Mark / Lampron, Lisa / Westover, Lori / Rhodes, Kenneth / Jackson, Paul F

Bioorganic & medicinal chemistry letters. 2013 May 1, v. 23, no. 9

2013

Abstract: A novel series of benzyl substituted thieno[2,3-d]pyrimidines were identified as potent A₂A receptor antagonists. Several five- and six-membered heterocyclic replacements for the optimized methylfuran were explored. Select compounds effectively reverse ... ...

Abstract	A novel series of benzyl substituted thieno[2,3-d]pyrimidines were identified as potent A₂A receptor antagonists. Several five- and six-membered heterocyclic replacements for the optimized methylfuran were explored. Select compounds effectively reverse catalepsy in mice when dosed orally.
Keywords	adenosine ; antagonists ; chemistry ; mice ; pyrimidines
Language	English
Dates of publication	2013-0501
Size	p. 2688-2691.
Publishing place	Elsevier Ltd
Document type	Article
ZDB-ID	1063195-1
ISSN	1464-3405 ; 0960-894X
ISSN (online)	1464-3405
ISSN	0960-894X
DOI	10.1016/j.bmcl.2013.02.078
Database	NAL-Catalogue (AGRICOLA)

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Article ; Online: Design and characterization of optimized adenosine A₂A/A₁ receptor antagonists for the treatment of Parkinson's disease.

Shook, Brian C / Rassnick, Stefanie / Wallace, Nathaniel / Crooke, Jeffrey / Ault, Mark / Chakravarty, Devraj / Barbay, J Kent / Wang, Aihua / Powell, Mark T / Leonard, Kristi / Alford, Vernon / Scannevin, Robert H / Carroll, Karen / Lampron, Lisa / Westover, Lori / Lim, Heng-Keang / Russell, Ronald / Branum, Shawn / Wells, Kenneth M /

Damon, Sandra / Youells, Scott / Li, Xun / Beauchamp, Derek A / Rhodes, Kenneth / Jackson, Paul F

Journal of medicinal chemistry

2012 Volume 55, Issue 3, Page(s) 1402–1417

Abstract: The design and characterization of two, dual adenosine A(2A)/A(1) receptor antagonists in several animal models of Parkinson's disease is described. Compound 1 was previously reported as a potential treatment for Parkinson's disease. Further ... ...

Abstract	The design and characterization of two, dual adenosine A(2A)/A(1) receptor antagonists in several animal models of Parkinson's disease is described. Compound 1 was previously reported as a potential treatment for Parkinson's disease. Further characterization of 1 revealed that it was metabolized to reactive intermediates that caused the genotoxicity of 1 in the Ames and mouse lymphoma L51784 assays. The identification of the metabolites enabled the preparation of two optimized compounds 13 and 14 that were devoid of the metabolic liabilities associated with 1. Compounds 13 and 14 are potent dual A(2A)/A(1) receptor antagonists that have excellent activity, after oral administration, across a number of animal models of Parkinson's disease including mouse and rat models of haloperidol-induced catalepsy, mouse and rat models of reserpine-induced akinesia, and the rat 6-hydroxydopamine (6-OHDA) lesion model of drug-induced rotation.
MeSH term(s)	Adenosine A1 Receptor Antagonists/chemical synthesis ; Adenosine A1 Receptor Antagonists/pharmacokinetics ; Adenosine A1 Receptor Antagonists/pharmacology ; Adenosine A2 Receptor Antagonists/chemical synthesis ; Adenosine A2 Receptor Antagonists/pharmacokinetics ; Adenosine A2 Receptor Antagonists/pharmacology ; Administration, Oral ; Animals ; Drug Design ; Female ; Indenes/chemical synthesis ; Indenes/pharmacokinetics ; Indenes/pharmacology ; Macaca fascicularis ; Male ; Mice ; Mice, Inbred BALB C ; Parkinsonian Disorders/chemically induced ; Parkinsonian Disorders/drug therapy ; Pyrimidines/chemical synthesis ; Pyrimidines/pharmacokinetics ; Pyrimidines/pharmacology ; Rats ; Rats, Sprague-Dawley ; Receptor, Adenosine A2A/metabolism ; Structure-Activity Relationship
Chemical Substances	2-amino-8-(2-morpholinoethoxy)-4-phenyl-5H-indeno(1,2-d)pyrimidin-5-one ; 2-amino-8-(4-methylpiperazine-1-carbonyl)-4-phenyl-5H-indeno(1,2-d)pyrimidin-5-one ; Adenosine A1 Receptor Antagonists ; Adenosine A2 Receptor Antagonists ; Indenes ; Pyrimidines ; Receptor, Adenosine A2A
Language	English
Publishing date	2012-02-09
Publishing country	United States
Document type	Journal Article
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/jm201640m
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Article ; Online: In vivo characterization of a dual adenosine A2A/A1 receptor antagonist in animal models of Parkinson's disease.

Shook, Brian C / Rassnick, Stefanie / Osborne, Melville C / Davis, Scott / Westover, Lori / Boulet, Jamie / Hall, Daniel / Rupert, Kenneth C / Heintzelman, Geoffrey R / Hansen, Kristin / Chakravarty, Devraj / Bullington, James L / Russell, Ronald / Branum, Shawn / Wells, Kenneth M / Damon, Sandra / Youells, Scott / Li, Xun / Beauchamp, Derek A /

Palmer, David / Reyes, Mayra / Demarest, Keith / Tang, Yuting / Rhodes, Kenneth / Jackson, Paul F

Journal of medicinal chemistry

2010 Volume 53, Issue 22, Page(s) 8104–8115

Abstract: The in vivo characterization of a dual adenosine A(2A)/A(1) receptor antagonist in several animal models of Parkinson's disease is described. Discovery and scale-up syntheses of compound 1 are described in detail, highlighting optimization steps that ... ...

Abstract	The in vivo characterization of a dual adenosine A(2A)/A(1) receptor antagonist in several animal models of Parkinson's disease is described. Discovery and scale-up syntheses of compound 1 are described in detail, highlighting optimization steps that increased the overall yield of 1 from 10.0% to 30.5%. Compound 1 is a potent A(2A)/A(1) receptor antagonist in vitro (A(2A) K(i) = 4.1 nM; A(1) K(i) = 17.0 nM) that has excellent activity, after oral administration, across a number of animal models of Parkinson's disease including mouse and rat models of haloperidol-induced catalepsy, mouse model of reserpine-induced akinesia, rat 6-hydroxydopamine (6-OHDA) lesion model of drug-induced rotation, and MPTP-treated non-human primate model.
MeSH term(s)	Adenosine A1 Receptor Antagonists/chemical synthesis ; Adenosine A1 Receptor Antagonists/pharmacokinetics ; Adenosine A1 Receptor Antagonists/pharmacology ; Adenosine A2 Receptor Antagonists/chemical synthesis ; Adenosine A2 Receptor Antagonists/pharmacokinetics ; Adenosine A2 Receptor Antagonists/pharmacology ; Administration, Oral ; Animals ; Antiparkinson Agents/chemical synthesis ; Antiparkinson Agents/pharmacokinetics ; Antiparkinson Agents/pharmacology ; Callithrix ; Disease Models, Animal ; Female ; Indenes/chemical synthesis ; Indenes/pharmacokinetics ; Indenes/pharmacology ; Macaca fascicularis ; Male ; Mice ; Mice, Inbred BALB C ; Parkinson Disease/metabolism ; Pyrimidines/chemical synthesis ; Pyrimidines/pharmacokinetics ; Pyrimidines/pharmacology ; Rats ; Rats, Sprague-Dawley ; Receptor, Adenosine A2A/physiology
Chemical Substances	2-amino-4-phenyl-8-(pyrrolidin-1-ylmethyl)-5H-indeno(1,2-d)pyrimidin-5-one ; Adenosine A1 Receptor Antagonists ; Adenosine A2 Receptor Antagonists ; Antiparkinson Agents ; Indenes ; Pyrimidines ; Receptor, Adenosine A2A
Language	English
Publishing date	2010-11-25
Publishing country	United States
Document type	Journal Article
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/jm100971t
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Article ; Online: Methylene amine substituted arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists.

Shook, Brian C / Rassnick, Stefanie / Hall, Daniel / Rupert, Kenneth C / Heintzelman, Geoffrey R / Hansen, Kristen / Chakravarty, Devraj / Bullington, James L / Scannevin, Robert H / Magliaro, Brian / Westover, Lori / Carroll, Karen / Lampron, Lisa / Russell, Ronald / Branum, Shawn / Wells, Kenneth / Damon, Sandra / Youells, Scott / Li, Xun /

Osbourne, Mel / Demarest, Keith / Tang, Yuting / Rhodes, Kenneth / Jackson, Paul F

Bioorganic & medicinal chemistry letters

2010 Volume 20, Issue 9, Page(s) 2864–2867

Abstract: A novel series of arylindenopyrimidines were identified as A(2A) and A(1) receptor antagonists. The series was optimized for in vitro activity by substituting the 8- and 9-positions with methylene amine substituents. The compounds show excellent activity ...

Abstract	A novel series of arylindenopyrimidines were identified as A(2A) and A(1) receptor antagonists. The series was optimized for in vitro activity by substituting the 8- and 9-positions with methylene amine substituents. The compounds show excellent activity in mouse models of Parkinson's disease when dosed orally.
MeSH term(s)	Adenosine A1 Receptor Antagonists ; Adenosine A2 Receptor Antagonists ; Amines/chemical synthesis ; Amines/chemistry ; Amines/therapeutic use ; Animals ; Catalepsy/drug therapy ; Disease Models, Animal ; Mice ; Neurotransmitter Agents/chemical synthesis ; Neurotransmitter Agents/chemistry ; Neurotransmitter Agents/therapeutic use ; Pyrimidines/chemical synthesis ; Pyrimidines/chemistry ; Pyrimidines/therapeutic use ; Receptor, Adenosine A1/metabolism ; Receptor, Adenosine A2A/metabolism ; Structure-Activity Relationship
Chemical Substances	Adenosine A1 Receptor Antagonists ; Adenosine A2 Receptor Antagonists ; Amines ; Neurotransmitter Agents ; Pyrimidines ; Receptor, Adenosine A1 ; Receptor, Adenosine A2A
Language	English
Publishing date	2010-05-01
Publishing country	England
Document type	Journal Article
ZDB-ID	1063195-1
ISSN	1464-3405 ; 0960-894X
ISSN (online)	1464-3405
ISSN	0960-894X
DOI	10.1016/j.bmcl.2010.03.042
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Article ; Online: Optimization of arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists.

Shook, Brian C / Rassnick, Stefanie / Chakravarty, Devraj / Wallace, Nathaniel / Ault, Mark / Crooke, Jeffrey / Barbay, J Kent / Wang, Aihua / Leonard, Kristi / Powell, Mark T / Alford, Vernon / Hall, Daniel / Rupert, Kenneth C / Heintzelman, Geoffrey R / Hansen, Kristen / Bullington, James L / Scannevin, Robert H / Carroll, Karen / Lampron, Lisa /

Westover, Lori / Russell, Ronald / Branum, Shawn / Wells, Kenneth / Damon, Sandra / Youells, Scott / Beauchamp, Derek / Li, Xun / Rhodes, Kenneth / Jackson, Paul F

Bioorganic & medicinal chemistry letters

2010 Volume 20, Issue 9, Page(s) 2868–2871

Abstract: Two reactive metabolites were identified in vivo for the dual A(2A)/A(1) receptor antagonist 1. Two strategies were implemented to successfully mitigate the metabolic liabilities associated with 1. Optimization of the arylindenopyrimidines led to a ... ...

Abstract	Two reactive metabolites were identified in vivo for the dual A(2A)/A(1) receptor antagonist 1. Two strategies were implemented to successfully mitigate the metabolic liabilities associated with 1. Optimization of the arylindenopyrimidines led to a number of amide, ether, and amino analogs having comparable in vitro and in vivo activity.
MeSH term(s)	Adenosine A1 Receptor Antagonists ; Adenosine A2 Receptor Antagonists ; Animals ; Catalepsy/drug therapy ; Disease Models, Animal ; Mice ; Neurotransmitter Agents/chemical synthesis ; Neurotransmitter Agents/chemistry ; Neurotransmitter Agents/therapeutic use ; Pyrimidines/chemical synthesis ; Pyrimidines/chemistry ; Pyrimidines/therapeutic use ; Receptor, Adenosine A1/metabolism ; Receptor, Adenosine A2A/metabolism ; Structure-Activity Relationship
Chemical Substances	Adenosine A1 Receptor Antagonists ; Adenosine A2 Receptor Antagonists ; Neurotransmitter Agents ; Pyrimidines ; Receptor, Adenosine A1 ; Receptor, Adenosine A2A
Language	English
Publishing date	2010-05-01
Publishing country	England
Document type	Journal Article
ZDB-ID	1063195-1
ISSN	1464-3405 ; 0960-894X
ISSN (online)	1464-3405
ISSN	0960-894X
DOI	10.1016/j.bmcl.2010.03.024
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Article: Substituted thieno[2,3-d]pyrimidines as adenosine A₂A receptor antagonists

Shook, Brian C. / Chakravarty, Devraj / Barbay, J. Kent / Wang, Aihua / Leonard, Kristi / Alford, Vernon / Powell, Mark T. / Rassnick, Stefanie / Scannevin, Robert H. / Carroll, Karen / Wallace, Nathaniel / Crooke, Jeffrey / Ault, Mark / Lampron, Lisa / Westover, Lori / Rhodes, Kenneth / Jackson, Paul F.

Bioorganic & medicinal chemistry letters

Volume v. 23,, Issue no. 9

Abstract	A novel series of benzyl substituted thieno[2,3-d]pyrimidines were identified as potent A₂A receptor antagonists. Several five- and six-membered heterocyclic replacements for the optimized methylfuran were explored. Select compounds effectively reverse catalepsy in mice when dosed orally.
Keywords	mice ; adenosine ; chemistry ; pyrimidines ; antagonists
Language	English
Document type	Article
ISSN	0960-894X
Database	AGRIS - International Information System for the Agricultural Sciences and Technology

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