Abstract
The design and synthesis of a series of new fluorescent coumarin-containing melatonin analogues is presented. The combination of high-binding affinities for human melatonergic receptors (h-MT₁R and h-MT₂R) and fluorescent properties, derived from the inclusion of melatonin pharmacophoric elements in the coumarin scaffold, yielded suitable candidates for the development of MT₁R and MT₂R fluorescent probes for imaging in biological media.
Keywords:
Bioisosterism; Coumarins; GPCRs fluorescent probes; Melatonin.
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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Coumarins / chemistry*
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Dose-Response Relationship, Drug
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Drug Design*
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Fluorescent Dyes / analysis
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Fluorescent Dyes / chemical synthesis*
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Fluorescent Dyes / chemistry*
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Humans
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Ligands
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Melatonin / chemistry*
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Melatonin / metabolism
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Molecular Imaging / methods
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Molecular Structure
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Receptor, Melatonin, MT1 / chemistry
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Receptor, Melatonin, MT1 / metabolism*
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Receptor, Melatonin, MT2 / chemistry
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Receptor, Melatonin, MT2 / metabolism*
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Structure-Activity Relationship
Substances
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Coumarins
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Fluorescent Dyes
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Ligands
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Receptor, Melatonin, MT1
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Receptor, Melatonin, MT2
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coumarin
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Melatonin