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2-Aryladenine Derivatives as a Potent Scaffold for Adenosine Receptor Antagonists : The 6-Morpholino Derivatives
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- Areias, Filipe (author)
- Univ Minho, Ctr Chem Univ Minho CQUM, Campus Gualtar, P-4710057 Braga, Portugal.;Univ Santiago De Compostela, Ctr Res Mol Med & Chron Dis CiMUS, Avda Barcelona, Santiago De Compostela 15782, Spain.;Yachay Tech Univ, Sch Chem Sci & Engn, Urcuqui 100119, Ecuador.
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- Correia, Carla (author)
- Univ Minho, Ctr Chem Univ Minho CQUM, Campus Gualtar, P-4710057 Braga, Portugal.
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- Rocha, Ashly (author)
- Univ Minho, Ctr Chem Univ Minho CQUM, Campus Gualtar, P-4710057 Braga, Portugal.
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- Univ Minho, Ctr Chem Univ Minho CQUM, Campus Gualtar, P-4710057 Braga, Portugal;Univ Santiago De Compostela, Ctr Res Mol Med & Chron Dis CiMUS, Avda Barcelona, Santiago De Compostela 15782, Spain.;Yachay Tech Univ, Sch Chem Sci & Engn, Urcuqui 100119, Ecuador. Univ Minho, Ctr Chem Univ Minho CQUM, Campus Gualtar, P-4710057 Braga, Portugal. (creator_code:org_t)
- MDPI, 2024
- 2024
- English.
- In: Molecules. - : MDPI. - 1431-5157 .- 1420-3049. ; 29:11
- Journal article (peer-reviewed)
Abstract
Subject headings
Close
- A set of 2-aryl-9-H or methyl-6-morpholinopurine derivatives were synthesized and assayed through radioligand binding tests at human A1, A2A, A2B, and A3 adenosine receptor subtypes. Eleven purines showed potent antagonism at A1, A3, dual A1/A2A, A1/A2B, or A1/A3 adenosine receptors. Additionally, three compounds showed high affinity without selectivity for any specific adenosine receptor. The structure-activity relationships were made for this group of new compounds. The 9-methylpurine derivatives were generally less potent but more selective, and the 9H-purine derivatives were more potent but less selective. These compounds can be an important source of new biochemical tools and/or pharmacological drugs.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmakologi och toxikologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmacology and Toxicology (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
Keyword
- G protein-coupled receptors
- adenine derivatives
- adenosine receptor antagonists
- 2-arylpurine derivatives
- structure-activity relationship
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- ref (subject category)
- art (subject category)
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