Use of molecular modeling aided design to dial out hERG liability in adenosine A2A receptor antagonists

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2015.05.036 ◽

2015 ◽

Vol 25 (15) ◽

pp. 2958-2962 ◽

Author(s):

Qiaolin Deng ◽

Yeon-Hee Lim ◽

Rajan Anand ◽

Younong Yu ◽

Jae-hun Kim ◽

...

Keyword(s):

Molecular Modeling ◽

Adenosine A2a Receptor ◽

Receptor Antagonists ◽

Adenosine A2a Receptor Antagonists ◽

A2a Receptor ◽

Aided Design ◽

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Adenosine A2A Receptor Antagonists in Parkinson’s Disease: Progress in Clinical Trials from the Newly Approved Istradefylline to Drugs in Early Development and Those Already Discontinued

CNS Drugs ◽

10.1007/s40263-014-0161-7 ◽

2014 ◽

Vol 28 (5) ◽

pp. 455-474 ◽

Author(s):

Annalisa Pinna

Keyword(s):

Parkinson’S Disease ◽

Parkinson's Disease ◽

Clinical Trials ◽

Early Development ◽

Adenosine A2a Receptor ◽

Receptor Antagonists ◽

Disease Progress ◽

Adenosine A2a Receptor Antagonists ◽

A2a Receptor ◽

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Characterization of the trigeminovascular actions of several adenosine A2A receptor antagonists in an in vivo rat model of migraine

The Journal of Headache and Pain ◽

10.1186/s10194-018-0867-x ◽

2018 ◽

Vol 19 (1) ◽

Author(s):

Kristian A. Haanes ◽

Alejandro Labastida-Ramírez ◽

Kayi Y. Chan ◽

René de Vries ◽

Brian Shook ◽

...

Keyword(s):

Rat Model ◽

Adenosine A2a Receptor ◽

Receptor Antagonists ◽

Adenosine A2a Receptor Antagonists ◽

A2a Receptor ◽

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The Controversial Role of Adenosine A2A Receptor Antagonists as Neuro-protective Agents

Current Medicinal Chemistry - Central Nervous System Agents ◽

10.2174/1568015043477577 ◽

2004 ◽

Vol 4 (1) ◽

pp. 35-45 ◽

Author(s):

Patrizia Popoli ◽

David Blum ◽

Annita Pintor ◽

Maria Tebano ◽

Claudio Frank ◽

...

Keyword(s):

Adenosine A2a Receptor ◽

Receptor Antagonists ◽

Protective Agents ◽

Adenosine A2a Receptor Antagonists ◽

A2a Receptor ◽

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Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A2A receptor antagonists

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2010.06.138 ◽

2010 ◽

Vol 20 (17) ◽

pp. 5241-5244 ◽

Author(s):

Anette Graven Sams ◽

Gitte Kobberøe Mikkelsen ◽

Mogens Larsen ◽

Lars Torup ◽

Lise Tøttrup Brennum ◽

...

Keyword(s):

Adenosine A2a Receptor ◽

Lead Optimization ◽

Receptor Antagonists ◽

Adenosine A2a Receptor Antagonists ◽

A2a Receptor ◽

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Synthetic studies on selective adenosine A2A receptor antagonists: Synthesis and structure–activity relationships of novel benzofuran derivatives

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2009.12.028 ◽

2010 ◽

Vol 20 (3) ◽

pp. 1090-1093 ◽

Author(s):

Osamu Saku ◽

Mayumi Saki ◽

Masako Kurokawa ◽

Ken Ikeda ◽

Takuya Takizawa ◽

...

Keyword(s):

Adenosine A2a Receptor ◽

Receptor Antagonists ◽

Structure Activity Relationships ◽

Structure Activity ◽

Adenosine A2a Receptor Antagonists ◽

A2a Receptor ◽

Synthetic Studies ◽

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The effects of adenosine A2A receptor antagonists on haloperidol-induced movement disorders in primates

Psychopharmacology ◽

10.1007/s00213-008-1214-8 ◽

2008 ◽

Vol 200 (3) ◽

pp. 393-401 ◽

Author(s):

Geoffrey B. Varty ◽

Robert A. Hodgson ◽

Annamarie J. Pond ◽

Michael E. Grzelak ◽

Eric M. Parker ◽

...

Keyword(s):

Movement Disorders ◽

Adenosine A2a Receptor ◽

Receptor Antagonists ◽

Adenosine A2a Receptor Antagonists ◽

A2a Receptor ◽

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Potential of Adenosine A2A Receptor Antagonists in the Treatment of Movement Disorders

CNS Drugs ◽

10.2165/00023210-199810050-00001 ◽

1998 ◽

Vol 10 (5) ◽

pp. 311-320 ◽

Author(s):

Judit Mally ◽

Trevor W. Stone

Keyword(s):

Movement Disorders ◽

Adenosine A2a Receptor ◽

Receptor Antagonists ◽

Adenosine A2a Receptor Antagonists ◽

A2a Receptor ◽

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Novel adenosine A2A receptor ligands: A synthetic, functional and computational investigation of selected literature adenosine A2A receptor antagonists for extending into extracellular space

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2013.03.070 ◽

2013 ◽

Vol 23 (11) ◽

pp. 3427-3433 ◽

Author(s):

Manuela Jörg ◽

Jeremy Shonberg ◽

Frankie S. Mak ◽

Neil D. Miller ◽

Elizabeth Yuriev ◽

...

Keyword(s):

Extracellular Space ◽

Adenosine A2a Receptor ◽

Computational Investigation ◽

Receptor Ligands ◽

Receptor Antagonists ◽

Adenosine A2a Receptor Antagonists ◽

A2a Receptor ◽

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ChemInform Abstract: Adenosine A2a Receptor Antagonists as Novel anti-Parkinsonian Agents: A Review of Structure-Activity Relationships

10.1002/chin.201011263 ◽

2010 ◽

Vol 41 (11) ◽

pp. no-no ◽

Author(s):

F. Azam ◽

I. A. Ibn-Rajab ◽

A. A. Alruiad

Keyword(s):

Adenosine A2a Receptor ◽

Receptor Antagonists ◽

Structure Activity Relationships ◽

Structure Activity ◽

Adenosine A2a Receptor Antagonists ◽

A2a Receptor ◽

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Adenosine A2A receptor antagonists prevent the increase in striatal glutamate levels induced by glutamate uptake inhibitors

Journal of Neurochemistry ◽

10.1111/j.1471-4159.2003.02306.x ◽

2004 ◽

Vol 89 (1) ◽

pp. 152-156 ◽

Author(s):

A. Pintor ◽

M. Galluzzo ◽

R. Grieco ◽

A. Pezzola ◽

R. Reggio ◽

...

Keyword(s):

Glutamate Uptake ◽

Adenosine A2a Receptor ◽

Receptor Antagonists ◽

Uptake Inhibitors ◽

Adenosine A2a Receptor Antagonists ◽

A2a Receptor ◽

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