Abstract
In this paper we describe an extension SAR study of pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine nucleus as A3AR antagonist. Our initial aim was to replace the phenylcarbamoyl moiety at the 5 position of PTP nucleus with a thiourea functionality to evaluate the contribution of new structural modification against the A3AR. The synthesized 12-25 were not characterized by the predicted side chain but by a 1,3-disubstituted guanidine and are shown to be interesting A3AR antagonists.
MeSH terms
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Animals
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Binding, Competitive
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CHO Cells
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Cricetulus
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Cyclic AMP / metabolism
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Drug Design*
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Humans
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Models, Molecular
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Molecular Structure
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Purinergic P1 Receptor Antagonists / chemistry*
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Purinergic P1 Receptor Antagonists / pharmacology*
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Pyrazoles / chemistry*
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Pyrimidines / chemistry*
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Radioligand Assay
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Receptor, Adenosine A3 / chemistry*
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Structure-Activity Relationship
Substances
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Purinergic P1 Receptor Antagonists
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Pyrazoles
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Pyrimidines
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Receptor, Adenosine A3
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Cyclic AMP