2-Aryladenine derivatives as a potent scaffold for A1, A3 and dual A1/A3 adenosine receptor antagonists: Synthesis and structure-activity relationships
[Display omitted] From a collection containing more than 1500 academic compounds, in silico screening identified a hit for the human A1 adenosine receptor containing a new purine scaffold. To study the structure activity relationships of this new chemical series for adenosine receptors, a library of...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry 2019-08, Vol.27 (16), p.3551-3558 |
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| container_issue | 16 |
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| container_title | Bioorganic & medicinal chemistry |
| container_volume | 27 |
| creator | Areias, Filipe Correia, Carla Rocha, Ashly Brea, José Castro, Marián Loza, Maria I. Proença, M. Fernanda Carvalho, M. Alice |
| description | [Display omitted]
From a collection containing more than 1500 academic compounds, in silico screening identified a hit for the human A1 adenosine receptor containing a new purine scaffold. To study the structure activity relationships of this new chemical series for adenosine receptors, a library of 24 purines was synthesized and tested in radioligand binding assays at human A1, A2A, A2B and A3 adenosine receptor subtypes. Fourteen molecules showed potent antagonism at A1, A3 or dual A1/A3 adenosine receptors. This purine scaffold is an important source for novel biochemical tools and/or therapeutic drugs. |
| doi_str_mv | 10.1016/j.bmc.2019.06.034 |
| format | Article |
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From a collection containing more than 1500 academic compounds, in silico screening identified a hit for the human A1 adenosine receptor containing a new purine scaffold. To study the structure activity relationships of this new chemical series for adenosine receptors, a library of 24 purines was synthesized and tested in radioligand binding assays at human A1, A2A, A2B and A3 adenosine receptor subtypes. Fourteen molecules showed potent antagonism at A1, A3 or dual A1/A3 adenosine receptors. This purine scaffold is an important source for novel biochemical tools and/or therapeutic drugs.</description><subject>2-Arylpurine derivatives</subject><subject>Adenine derivatives</subject><subject>Adenosine receptor antagonists</subject><issn>0968-0896</issn><issn>1464-3391</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2019</creationdate><recordtype>article</recordtype><recordid>eNp9kc-KFDEQxoMoOK4-gLccPdi9lXQn262nYfEfLHhQzyGdVLsZepI2lR6YJ_F1zTiehYKi4Pt9RdXH2GsBrQChbw_tdHStBDG2oFvo-idsJ3rdN103iqdsB6MeGhhG_Zy9IDoAgOxHsWO_ZbPP58V6jCEi95jDyZZwQuK2Fl9TwVg4OTvPafF8TpnvxVu-77iNnvvNLnW-vYzVItHFJKPDtVShjcX-TDFQoXf82zmWR6RAf0EqeXNly9hYV9eFcq7YUjenSI9hpZfs2WwXwlf_-g378fHD9_vPzcPXT1_u9w-N65QqDYrhTikJCryq94xDP0x3QnXWqUFPo568dJOyFrSfnUCNvVRiQO201_0spu6Gvbn6rjn92pCKOQZyuCw2YtrISKm6QaoRoErFVepyIso4mzWHo81nI8BcQjAHU0MwlxAMaFNDqMz7K4P1hlPAbMgFjA59qF8qxqfwH_oPCSmQ3A</recordid><startdate>20190815</startdate><enddate>20190815</enddate><creator>Areias, Filipe</creator><creator>Correia, Carla</creator><creator>Rocha, Ashly</creator><creator>Brea, José</creator><creator>Castro, Marián</creator><creator>Loza, Maria I.</creator><creator>Proença, M. Fernanda</creator><creator>Carvalho, M. Alice</creator><general>Elsevier Ltd</general><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>20190815</creationdate><title>2-Aryladenine derivatives as a potent scaffold for A1, A3 and dual A1/A3 adenosine receptor antagonists: Synthesis and structure-activity relationships</title><author>Areias, Filipe ; Correia, Carla ; Rocha, Ashly ; Brea, José ; Castro, Marián ; Loza, Maria I. ; Proença, M. Fernanda ; Carvalho, M. Alice</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c355t-e187552050d54919848b7153ac586b96bd2cb5aa06dfc1e6e42518e6c6d64f1b3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2019</creationdate><topic>2-Arylpurine derivatives</topic><topic>Adenine derivatives</topic><topic>Adenosine receptor antagonists</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Areias, Filipe</creatorcontrib><creatorcontrib>Correia, Carla</creatorcontrib><creatorcontrib>Rocha, Ashly</creatorcontrib><creatorcontrib>Brea, José</creatorcontrib><creatorcontrib>Castro, Marián</creatorcontrib><creatorcontrib>Loza, Maria I.</creatorcontrib><creatorcontrib>Proença, M. Fernanda</creatorcontrib><creatorcontrib>Carvalho, M. Alice</creatorcontrib><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Bioorganic & medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Areias, Filipe</au><au>Correia, Carla</au><au>Rocha, Ashly</au><au>Brea, José</au><au>Castro, Marián</au><au>Loza, Maria I.</au><au>Proença, M. Fernanda</au><au>Carvalho, M. Alice</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>2-Aryladenine derivatives as a potent scaffold for A1, A3 and dual A1/A3 adenosine receptor antagonists: Synthesis and structure-activity relationships</atitle><jtitle>Bioorganic & medicinal chemistry</jtitle><date>2019-08-15</date><risdate>2019</risdate><volume>27</volume><issue>16</issue><spage>3551</spage><epage>3558</epage><pages>3551-3558</pages><issn>0968-0896</issn><eissn>1464-3391</eissn><abstract>[Display omitted]
From a collection containing more than 1500 academic compounds, in silico screening identified a hit for the human A1 adenosine receptor containing a new purine scaffold. To study the structure activity relationships of this new chemical series for adenosine receptors, a library of 24 purines was synthesized and tested in radioligand binding assays at human A1, A2A, A2B and A3 adenosine receptor subtypes. Fourteen molecules showed potent antagonism at A1, A3 or dual A1/A3 adenosine receptors. This purine scaffold is an important source for novel biochemical tools and/or therapeutic drugs.</abstract><pub>Elsevier Ltd</pub><doi>10.1016/j.bmc.2019.06.034</doi><tpages>8</tpages><oa>free_for_read</oa></addata></record> |
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| ispartof | Bioorganic & medicinal chemistry, 2019-08, Vol.27 (16), p.3551-3558 |
| issn | 0968-0896 1464-3391 |
| language | eng |
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| source | Elsevier ScienceDirect Journals |
| subjects | 2-Arylpurine derivatives Adenine derivatives Adenosine receptor antagonists |
| title | 2-Aryladenine derivatives as a potent scaffold for A1, A3 and dual A1/A3 adenosine receptor antagonists: Synthesis and structure-activity relationships |
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