Literature DB >> 18411049

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 Gillespie1, 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.   

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.

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Year:  2008        PMID： 18411049     DOI： 10.1016/j.bmcl.2008.03.072

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  11 in total

1.  Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor.

Authors:  Chris de Graaf; Albert J Kooistra; Henry F Vischer; Vsevolod Katritch; Martien Kuijer; Mitsunori Shiroishi; So Iwata; Tatsuro Shimamura; Raymond C Stevens; Iwan J P de Esch; Rob Leurs
Journal:  J Med Chem       Date:  2011-11-07       Impact factor: 7.446

Review 2.  Introduction to adenosine receptors as therapeutic targets.

Authors:  Kenneth A Jacobson
Journal:  Handb Exp Pharmacol       Date:  2009

Review 3.  Adenosine A(2A) Receptor Antagonists and Parkinson's Disease.

Authors:  Brian C Shook; Paul F Jackson
Journal:  ACS Chem Neurosci       Date:  2011-06-21       Impact factor: 4.418

4.  Novel pyrazolo[3,4-d]pyrimidine derivatives as potential antitumor agents: exploratory synthesis, preliminary structure-activity relationships, and in vitro biological evaluation.

Authors:  Hai-Yun He; Jin-Ni Zhao; Ruo Jia; Ying-Lan Zhao; Sheng-Yong Yang; Luo-Ting Yu; Li Yang
Journal:  Molecules       Date:  2011-12-20       Impact factor: 4.411

5.  Development of 18F-Labeled Radiotracers for PET Imaging of the Adenosine A2A Receptor: Synthesis, Radiolabeling and Preliminary Biological Evaluation.

Authors:  Thu Hang Lai; Susann Schröder; Magali Toussaint; Sladjana Dukić-Stefanović; Mathias Kranz; Friedrich-Alexander Ludwig; Steffen Fischer; Jörg Steinbach; Winnie Deuther-Conrad; Peter Brust; Rareş-Petru Moldovan
Journal:  Int J Mol Sci       Date:  2021-02-25       Impact factor: 5.923

Review 6.  Adenosine-A2A Receptor Pathway in Cancer Immunotherapy.

Authors:  Changfa Sun; Bochu Wang; Shilei Hao
Journal:  Front Immunol       Date:  2022-03-21       Impact factor: 7.561

7.  Combinatorial delivery of CPI444 and vatalanib loaded on PEGylated graphene oxide as an effective nanoformulation to target glioblastoma multiforme: In vitro evaluation.

Authors:  Vishnu S Mishra; Sachin Patil; Puli Chandramouli Reddy; Bimlesh Lochab
Journal:  Front Oncol       Date:  2022-08-16       Impact factor: 5.738

Review 8.  Pyrazolo derivatives as potent adenosine receptor antagonists: an overview on the structure-activity relationships.

Authors:  Siew Lee Cheong; Gopalakrishnan Venkatesan; Priyankar Paira; Ramasamy Jothibasu; Alexander Laurence Mandel; Stephanie Federico; Giampiero Spalluto; Giorgia Pastorin
Journal:  Int J Med Chem       Date:  2011-03-07

9.  Acetylcholinesterase enzyme inhibitor activity of some novel pyrazinamide condensed 1,2,3,4-tetrahydropyrimidines.

Authors:  Karthikeyan Elumalai; Mohammed Ashraf Ali; Manogaran Elumalai; Kalpana Eluri; Sivaneswari Srinivasan
Journal:  Biotechnol Rep (Amst)       Date:  2014-10-29

10.  Design, practical synthesis, and biological evaluation of novel 6-(pyrazolylmethyl)-4-quinoline-3-carboxylic acid derivatives as HIV-1 integrase inhibitors.

Authors:  Liming Hu; Song Yan; Zaigang Luo; Xiao Han; Yujie Wang; Zhanyang Wang; Chengchu Zeng
Journal:  Molecules       Date:  2012-09-06       Impact factor: 4.411
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