Abstract
In the aim of identifying new privileged structures, we describe the 5-steps synthesis of cyclic guanidine compounds "tetrahydroisoquinoline-iminoimidazolines" derived from tetrahydroisoquinoline-hydantoin core. In order to evaluate this new minimal structure and the impact of replacing a carbonyle by a guanidine moiety, their affinity towards adenosine receptor A2A was evaluated and compared to those of tetrahydroisoquinoline-hydantoin compounds.
Keywords:
A(2A) receptor; Guanidines; Iminoimidazoline; Privileged structure.
Copyright © 2015 Elsevier Masson SAS. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Dose-Response Relationship, Drug
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Drug Design*
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HEK293 Cells
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Humans
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Imidazolines / chemical synthesis
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Imidazolines / chemistry
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Imidazolines / pharmacology*
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Models, Molecular
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Molecular Structure
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Purinergic P1 Receptor Antagonists / chemical synthesis*
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Purinergic P1 Receptor Antagonists / chemistry
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Purinergic P1 Receptor Antagonists / pharmacology*
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Receptor, Adenosine A2A / metabolism*
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Structure-Activity Relationship
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Tetrahydroisoquinolines / chemical synthesis
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Tetrahydroisoquinolines / chemistry
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Tetrahydroisoquinolines / pharmacology*
Substances
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Imidazolines
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Purinergic P1 Receptor Antagonists
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Receptor, Adenosine A2A
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Tetrahydroisoquinolines