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Coumarins and adenosine receptors: New perceptions in structure–affinity relationships
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| Zeitschriftentitel: | Chemical Biology & Drug Design |
|---|---|
| Personen und Körperschaften: | , , , , , , |
| In: | Chemical Biology & Drug Design, 91, 2018, 1, S. 245-256 |
| Format: | E-Article |
| Sprache: | Englisch |
| veröffentlicht: |
Wiley
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| Schlagwörter: |
| author_facet |
Fonseca, André Matos, Maria João Vilar, Santiago Kachler, Sonja Klotz, Karl‐Norbert Uriarte, Eugenio Borges, Fernanda Fonseca, André Matos, Maria João Vilar, Santiago Kachler, Sonja Klotz, Karl‐Norbert Uriarte, Eugenio Borges, Fernanda |
|---|---|
| author |
Fonseca, André Matos, Maria João Vilar, Santiago Kachler, Sonja Klotz, Karl‐Norbert Uriarte, Eugenio Borges, Fernanda |
| spellingShingle |
Fonseca, André Matos, Maria João Vilar, Santiago Kachler, Sonja Klotz, Karl‐Norbert Uriarte, Eugenio Borges, Fernanda Chemical Biology & Drug Design Coumarins and adenosine receptors: New perceptions in structure–affinity relationships Molecular Medicine Biochemistry Drug Discovery Pharmacology Organic Chemistry |
| author_sort |
fonseca, andré |
| spelling |
Fonseca, André Matos, Maria João Vilar, Santiago Kachler, Sonja Klotz, Karl‐Norbert Uriarte, Eugenio Borges, Fernanda 1747-0277 1747-0285 Wiley Molecular Medicine Biochemistry Drug Discovery Pharmacology Organic Chemistry http://dx.doi.org/10.1111/cbdd.13075 <jats:p>Adenosine receptor (<jats:styled-content style="fixed-case">AR</jats:styled-content>) subtypes are involved in several physiological and pharmacological processes. Ligands that are able to selectively modulate one receptor subtype can delay or slow down the progression of diverse diseases. In this context, our research group focused its investigation into the discovery and development of novel, potent and selective <jats:styled-content style="fixed-case">AR</jats:styled-content> ligands based on coumarin scaffold. Therefore, a series of 3‐phenylcarboxamidocoumarins were synthesized and their affinity for the human <jats:styled-content style="fixed-case">AR</jats:styled-content> subtypes was screened by radioligand binding assays for A<jats:sub>1</jats:sub>, A<jats:sub>2A</jats:sub> and A<jats:sub>3</jats:sub> receptors and for A<jats:sub>2B</jats:sub> by adenylyl cyclase assay. Compound <jats:bold>26</jats:bold> was found to be the most remarkable, with a <jats:styled-content style="fixed-case"><jats:italic>h</jats:italic>A</jats:styled-content><jats:sub>1</jats:sub>/<jats:styled-content style="fixed-case"><jats:italic>h</jats:italic>A</jats:styled-content><jats:sub>3</jats:sub> and <jats:styled-content style="fixed-case"><jats:italic>h</jats:italic>A</jats:styled-content><jats:sub>2A</jats:sub>/<jats:styled-content style="fixed-case"><jats:italic>h</jats:italic>A</jats:styled-content><jats:sub>3</jats:sub> selectivity of 42, for the A<jats:sub>3</jats:sub> <jats:styled-content style="fixed-case">AR</jats:styled-content> (<jats:italic>K</jats:italic><jats:sub>i</jats:sub> = 2.4 μ<jats:sc>m</jats:sc>). Receptor‐driven molecular modelling studies have provided valuable information on the binding/selectivity data of compound <jats:bold>26</jats:bold> and for the following optimization process. Moreover, compound <jats:bold>26</jats:bold> presents drug‐like properties according to the general guidelines linked to the concept.</jats:p> Coumarins and adenosine receptors: New perceptions in structure–affinity relationships Chemical Biology & Drug Design |
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10.1111/cbdd.13075 |
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Online |
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Chemical Biology & Drug Design |
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| title |
Coumarins and adenosine receptors: New perceptions in structure–affinity relationships |
| title_unstemmed |
Coumarins and adenosine receptors: New perceptions in structure–affinity relationships |
| title_full |
Coumarins and adenosine receptors: New perceptions in structure–affinity relationships |
| title_fullStr |
Coumarins and adenosine receptors: New perceptions in structure–affinity relationships |
| title_full_unstemmed |
Coumarins and adenosine receptors: New perceptions in structure–affinity relationships |
| title_short |
Coumarins and adenosine receptors: New perceptions in structure–affinity relationships |
| title_sort |
coumarins and adenosine receptors: new perceptions in structure–affinity relationships |
| topic |
Molecular Medicine Biochemistry Drug Discovery Pharmacology Organic Chemistry |
| url |
http://dx.doi.org/10.1111/cbdd.13075 |
| publishDate |
2018 |
| physical |
245-256 |
| description |
<jats:p>Adenosine receptor (<jats:styled-content style="fixed-case">AR</jats:styled-content>) subtypes are involved in several physiological and pharmacological processes. Ligands that are able to selectively modulate one receptor subtype can delay or slow down the progression of diverse diseases. In this context, our research group focused its investigation into the discovery and development of novel, potent and selective <jats:styled-content style="fixed-case">AR</jats:styled-content> ligands based on coumarin scaffold. Therefore, a series of 3‐phenylcarboxamidocoumarins were synthesized and their affinity for the human <jats:styled-content style="fixed-case">AR</jats:styled-content> subtypes was screened by radioligand binding assays for A<jats:sub>1</jats:sub>, A<jats:sub>2A</jats:sub> and A<jats:sub>3</jats:sub> receptors and for A<jats:sub>2B</jats:sub> by adenylyl cyclase assay. Compound <jats:bold>26</jats:bold> was found to be the most remarkable, with a <jats:styled-content style="fixed-case"><jats:italic>h</jats:italic>A</jats:styled-content><jats:sub>1</jats:sub>/<jats:styled-content style="fixed-case"><jats:italic>h</jats:italic>A</jats:styled-content><jats:sub>3</jats:sub> and <jats:styled-content style="fixed-case"><jats:italic>h</jats:italic>A</jats:styled-content><jats:sub>2A</jats:sub>/<jats:styled-content style="fixed-case"><jats:italic>h</jats:italic>A</jats:styled-content><jats:sub>3</jats:sub> selectivity of 42, for the A<jats:sub>3</jats:sub> <jats:styled-content style="fixed-case">AR</jats:styled-content> (<jats:italic>K</jats:italic><jats:sub>i</jats:sub> = 2.4 μ<jats:sc>m</jats:sc>). Receptor‐driven molecular modelling studies have provided valuable information on the binding/selectivity data of compound <jats:bold>26</jats:bold> and for the following optimization process. Moreover, compound <jats:bold>26</jats:bold> presents drug‐like properties according to the general guidelines linked to the concept.</jats:p> |
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| author | Fonseca, André, Matos, Maria João, Vilar, Santiago, Kachler, Sonja, Klotz, Karl‐Norbert, Uriarte, Eugenio, Borges, Fernanda |
| author_facet | Fonseca, André, Matos, Maria João, Vilar, Santiago, Kachler, Sonja, Klotz, Karl‐Norbert, Uriarte, Eugenio, Borges, Fernanda, Fonseca, André, Matos, Maria João, Vilar, Santiago, Kachler, Sonja, Klotz, Karl‐Norbert, Uriarte, Eugenio, Borges, Fernanda |
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| description | <jats:p>Adenosine receptor (<jats:styled-content style="fixed-case">AR</jats:styled-content>) subtypes are involved in several physiological and pharmacological processes. Ligands that are able to selectively modulate one receptor subtype can delay or slow down the progression of diverse diseases. In this context, our research group focused its investigation into the discovery and development of novel, potent and selective <jats:styled-content style="fixed-case">AR</jats:styled-content> ligands based on coumarin scaffold. Therefore, a series of 3‐phenylcarboxamidocoumarins were synthesized and their affinity for the human <jats:styled-content style="fixed-case">AR</jats:styled-content> subtypes was screened by radioligand binding assays for A<jats:sub>1</jats:sub>, A<jats:sub>2A</jats:sub> and A<jats:sub>3</jats:sub> receptors and for A<jats:sub>2B</jats:sub> by adenylyl cyclase assay. Compound <jats:bold>26</jats:bold> was found to be the most remarkable, with a <jats:styled-content style="fixed-case"><jats:italic>h</jats:italic>A</jats:styled-content><jats:sub>1</jats:sub>/<jats:styled-content style="fixed-case"><jats:italic>h</jats:italic>A</jats:styled-content><jats:sub>3</jats:sub> and <jats:styled-content style="fixed-case"><jats:italic>h</jats:italic>A</jats:styled-content><jats:sub>2A</jats:sub>/<jats:styled-content style="fixed-case"><jats:italic>h</jats:italic>A</jats:styled-content><jats:sub>3</jats:sub> selectivity of 42, for the A<jats:sub>3</jats:sub> <jats:styled-content style="fixed-case">AR</jats:styled-content> (<jats:italic>K</jats:italic><jats:sub>i</jats:sub> = 2.4 μ<jats:sc>m</jats:sc>). Receptor‐driven molecular modelling studies have provided valuable information on the binding/selectivity data of compound <jats:bold>26</jats:bold> and for the following optimization process. Moreover, compound <jats:bold>26</jats:bold> presents drug‐like properties according to the general guidelines linked to the concept.</jats:p> |
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| spelling | Fonseca, André Matos, Maria João Vilar, Santiago Kachler, Sonja Klotz, Karl‐Norbert Uriarte, Eugenio Borges, Fernanda 1747-0277 1747-0285 Wiley Molecular Medicine Biochemistry Drug Discovery Pharmacology Organic Chemistry http://dx.doi.org/10.1111/cbdd.13075 <jats:p>Adenosine receptor (<jats:styled-content style="fixed-case">AR</jats:styled-content>) subtypes are involved in several physiological and pharmacological processes. Ligands that are able to selectively modulate one receptor subtype can delay or slow down the progression of diverse diseases. In this context, our research group focused its investigation into the discovery and development of novel, potent and selective <jats:styled-content style="fixed-case">AR</jats:styled-content> ligands based on coumarin scaffold. Therefore, a series of 3‐phenylcarboxamidocoumarins were synthesized and their affinity for the human <jats:styled-content style="fixed-case">AR</jats:styled-content> subtypes was screened by radioligand binding assays for A<jats:sub>1</jats:sub>, A<jats:sub>2A</jats:sub> and A<jats:sub>3</jats:sub> receptors and for A<jats:sub>2B</jats:sub> by adenylyl cyclase assay. Compound <jats:bold>26</jats:bold> was found to be the most remarkable, with a <jats:styled-content style="fixed-case"><jats:italic>h</jats:italic>A</jats:styled-content><jats:sub>1</jats:sub>/<jats:styled-content style="fixed-case"><jats:italic>h</jats:italic>A</jats:styled-content><jats:sub>3</jats:sub> and <jats:styled-content style="fixed-case"><jats:italic>h</jats:italic>A</jats:styled-content><jats:sub>2A</jats:sub>/<jats:styled-content style="fixed-case"><jats:italic>h</jats:italic>A</jats:styled-content><jats:sub>3</jats:sub> selectivity of 42, for the A<jats:sub>3</jats:sub> <jats:styled-content style="fixed-case">AR</jats:styled-content> (<jats:italic>K</jats:italic><jats:sub>i</jats:sub> = 2.4 μ<jats:sc>m</jats:sc>). Receptor‐driven molecular modelling studies have provided valuable information on the binding/selectivity data of compound <jats:bold>26</jats:bold> and for the following optimization process. Moreover, compound <jats:bold>26</jats:bold> presents drug‐like properties according to the general guidelines linked to the concept.</jats:p> Coumarins and adenosine receptors: New perceptions in structure–affinity relationships Chemical Biology & Drug Design |
| spellingShingle | Fonseca, André, Matos, Maria João, Vilar, Santiago, Kachler, Sonja, Klotz, Karl‐Norbert, Uriarte, Eugenio, Borges, Fernanda, Chemical Biology & Drug Design, Coumarins and adenosine receptors: New perceptions in structure–affinity relationships, Molecular Medicine, Biochemistry, Drug Discovery, Pharmacology, Organic Chemistry |
| title | Coumarins and adenosine receptors: New perceptions in structure–affinity relationships |
| title_full | Coumarins and adenosine receptors: New perceptions in structure–affinity relationships |
| title_fullStr | Coumarins and adenosine receptors: New perceptions in structure–affinity relationships |
| title_full_unstemmed | Coumarins and adenosine receptors: New perceptions in structure–affinity relationships |
| title_short | Coumarins and adenosine receptors: New perceptions in structure–affinity relationships |
| title_sort | coumarins and adenosine receptors: new perceptions in structure–affinity relationships |
| title_unstemmed | Coumarins and adenosine receptors: New perceptions in structure–affinity relationships |
| topic | Molecular Medicine, Biochemistry, Drug Discovery, Pharmacology, Organic Chemistry |
| url | http://dx.doi.org/10.1111/cbdd.13075 |