Abstract
Compilation of agmatine structure and imidazoline ring leads to a new family of imidazoline/alpha(2)-adrenoceptor ligands, 4(5)-(2-aminoethyl)imidazoline derivatives. Constraining of the guanidine moiety into heterocyclic ring improved the affinities of the resultant fusion compounds in comparison to agmatine itself. In this work, the synthetic approach and results for I(1), I(2), and alpha(2)-adrenoceptors affinities are reported.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Agmatine / analogs & derivatives*
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Agmatine / pharmacology
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Chemistry, Pharmaceutical / methods*
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Clonidine / pharmacology
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Drug Design
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Drug Evaluation, Preclinical
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Guanidine / chemistry
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Humans
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Imidazoles
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Imidazoline Receptors / chemistry*
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Imidazoline Receptors / metabolism
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Inhibitory Concentration 50
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Kinetics
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Models, Chemical
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Protein Binding
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Receptors, Adrenergic, alpha-2 / metabolism
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Recombinant Fusion Proteins / chemistry
Substances
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Imidazoles
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Imidazoline Receptors
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Receptors, Adrenergic, alpha-2
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Recombinant Fusion Proteins
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Agmatine
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Guanidine
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Clonidine