Evidence map›Paper›PMID 25954519›Full record

ReviewInternational journal of medicinal chemistry2011

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

Siew Lee Cheong, Gopalakrishnan Venkatesan, Priyankar Paira, Ramasamy Jothibasu, Alexander Laurence Mandel, Stephanie Federico, Giampiero Spalluto, Giorgia Pastorin

Abstract readReview
In one paragraph

Review in International journal of medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

1 citing paper in PubMed.

  1. Discovery of a High Affinity Adenosine AACS medicinal chemistry letters · 2022
    Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

8 authors.

Siew Lee CheongDepartment of Pharmacy, National University of Singapore, 3 Science Drive 2, Singapore 117543.
Gopalakrishnan VenkatesanDepartment of Pharmacy, National University of Singapore, 3 Science Drive 2, Singapore 117543.
Priyankar PairaDepartment of Pharmacy, National University of Singapore, 3 Science Drive 2, Singapore 117543.
Ramasamy JothibasuDepartment of Pharmacy, National University of Singapore, 3 Science Drive 2, Singapore 117543.
Alexander Laurence MandelDepartment of Pharmacy, National University of Singapore, 3 Science Drive 2, Singapore 117543.
Stephanie FedericoDipartimento di Scienze Farmaceutiche, Università degli Studi di Trieste, Piazzale Europa 1, 34127 Trieste, Italy.
Giampiero SpallutoDipartimento di Scienze Farmaceutiche, Università degli Studi di Trieste, Piazzale Europa 1, 34127 Trieste, Italy.
Giorgia PastorinDepartment of Pharmacy, National University of Singapore, 3 Science Drive 2, Singapore 117543.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

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.

Identifiers

PMID25954519
PMCPMC4411897

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Registered trials

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.