Pyrazolo Derivatives as Potent Adenosine Receptor Antagonists : An Overview on the Structure-Activity Relationships
Joint Authors
Federico, Stephanie
Venkatesan, Gopalakrishnan
Jothibasu, Ramasamy
Mandel, Alexander Laurence
Pastorin, Giorgia
Cheong, Siew Lee
Spalluto, Giampiero
Paira, Priyankar
Source
International Journal of Medicinal Chemistry
Issue
Vol. 2011, Issue 2011 (31 Dec. 2011), pp.1-15, 15 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2011-04-07
Country of Publication
Egypt
No. of Pages
15
Main Subjects
Abstract EN
In the past few decades, medicinal chemistry research towards potent and selective antagonists of human adenosine receptors (namely, A1, A2A, A2B, and A3) has been evolving rapidly.
These antagonists are deemed therapeutically beneficial in several pathological conditions including neurological and renal disorders, cancer, inflammation, and glaucoma.
Up to this point, many classes of compounds have been successfully synthesized and identified as potent human adenosine receptor antagonists.
In this paper, an overview of the structure-activity relationship (SAR) profiles of promising nonxanthine pyrazolo derivatives is reported and discussed.
We have emphasized the SAR for some representative structures such as pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]pyrimidines; pyrazolo-[3,4-c] or -[4,3-c]quinolines; pyrazolo-[4,3-d]pyrimidinones; pyrazolo-[3,4-d]pyrimidines and pyrazolo-[1,5-a]pyridines.
This overview not only clarifies the structural requirements deemed essential for affinity towards individual adenosine receptor subtypes, but it also sheds light on the rational design and optimization of existing structural templates to allow us to conceive new, more potent adenosine receptor antagonists.
American Psychological Association (APA)
Cheong, Siew Lee& Venkatesan, Gopalakrishnan& Paira, Priyankar& Jothibasu, Ramasamy& Mandel, Alexander Laurence& Federico, Stephanie…[et al.]. 2011. Pyrazolo Derivatives as Potent Adenosine Receptor Antagonists : An Overview on the Structure-Activity Relationships. International Journal of Medicinal Chemistry،Vol. 2011, no. 2011, pp.1-15.
https://search.emarefa.net/detail/BIM-474922
Modern Language Association (MLA)
Cheong, Siew Lee…[et al.]. Pyrazolo Derivatives as Potent Adenosine Receptor Antagonists : An Overview on the Structure-Activity Relationships. International Journal of Medicinal Chemistry No. 2011 (2011), pp.1-15.
https://search.emarefa.net/detail/BIM-474922
American Medical Association (AMA)
Cheong, Siew Lee& Venkatesan, Gopalakrishnan& Paira, Priyankar& Jothibasu, Ramasamy& Mandel, Alexander Laurence& Federico, Stephanie…[et al.]. Pyrazolo Derivatives as Potent Adenosine Receptor Antagonists : An Overview on the Structure-Activity Relationships. International Journal of Medicinal Chemistry. 2011. Vol. 2011, no. 2011, pp.1-15.
https://search.emarefa.net/detail/BIM-474922
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-474922