دورية أكاديمية
أعرض في EDS

2-Aryladenine Derivatives as a Potent Scaffold for Adenosine Receptor Antagonists: The 6-Morpholino Derivatives.

التفاصيل البيبلوغرافية
العنوان: 2-Aryladenine Derivatives as a Potent Scaffold for Adenosine Receptor Antagonists: The 6-Morpholino Derivatives.
المؤلفون: Areias F; Centre of Chemistry of University of Minho (CQUM), Campus de Gualtar, Universidade do Minho, 4710-057 Braga, Portugal.; Center for Research in Molecular Medicine and Chronic Diseases (CiMUS), Universidade de Santiago de Compostela, Avda de Barcelona, E-15782 Santiago de Compostela, Spain.; School of Chemical Sciences & Engineering, Yachay Tech University, Yachay City of Knowledge, Urcuqui 100119, Ecuador., Correia C; Centre of Chemistry of University of Minho (CQUM), Campus de Gualtar, Universidade do Minho, 4710-057 Braga, Portugal., Rocha A; Centre of Chemistry of University of Minho (CQUM), Campus de Gualtar, Universidade do Minho, 4710-057 Braga, Portugal., Teixeira S; Centre of Chemistry of University of Minho (CQUM), Campus de Gualtar, Universidade do Minho, 4710-057 Braga, Portugal., Castro M; Center for Research in Molecular Medicine and Chronic Diseases (CiMUS), Universidade de Santiago de Compostela, Avda de Barcelona, E-15782 Santiago de Compostela, Spain.; Instituto de Investigación Sanitaria de Santiago de Compostela (IDIS), Travesía da Choupana s/n, E-15706 Santiago de Compostela, Spain., Brea J; Center for Research in Molecular Medicine and Chronic Diseases (CiMUS), Universidade de Santiago de Compostela, Avda de Barcelona, E-15782 Santiago de Compostela, Spain.; Instituto de Investigación Sanitaria de Santiago de Compostela (IDIS), Travesía da Choupana s/n, E-15706 Santiago de Compostela, Spain., Hu H; Science for Life Laboratory, Department of Cell and Molecular Biology, Uppsala University, SE-75124 Uppsala, Sweden., Carlsson J; Science for Life Laboratory, Department of Cell and Molecular Biology, Uppsala University, SE-75124 Uppsala, Sweden., Loza MI; Center for Research in Molecular Medicine and Chronic Diseases (CiMUS), Universidade de Santiago de Compostela, Avda de Barcelona, E-15782 Santiago de Compostela, Spain.; Instituto de Investigación Sanitaria de Santiago de Compostela (IDIS), Travesía da Choupana s/n, E-15706 Santiago de Compostela, Spain., Proença MF; Centre of Chemistry of University of Minho (CQUM), Campus de Gualtar, Universidade do Minho, 4710-057 Braga, Portugal., Carvalho MA; Centre of Chemistry of University of Minho (CQUM), Campus de Gualtar, Universidade do Minho, 4710-057 Braga, Portugal.
المصدر: Molecules (Basel, Switzerland) [Molecules] 2024 May 28; Vol. 29 (11). Date of Electronic Publication: 2024 May 28.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: MDPI Country of Publication: Switzerland NLM ID: 100964009 Publication Model: Electronic Cited Medium: Internet ISSN: 1420-3049 (Electronic) Linking ISSN: 14203049 NLM ISO Abbreviation: Molecules Subsets: MEDLINE
أسماء مطبوعة: Original Publication: Basel, Switzerland : MDPI, c1995-
مواضيع طبية MeSH: Purinergic P1 Receptor Antagonists*/pharmacology , Purinergic P1 Receptor Antagonists*/chemistry, Humans ; Structure-Activity Relationship ; Receptors, Purinergic P1/metabolism ; Molecular Structure ; Adenine/analogs & derivatives ; Adenine/chemistry ; Adenine/pharmacology ; Morpholines/chemistry ; Morpholines/pharmacology ; Purines/chemistry ; Purines/pharmacology ; Purines/chemical synthesis ; CHO Cells
مستخلص: A set of 2-aryl-9-H or methyl-6-morpholinopurine derivatives were synthesized and assayed through radioligand binding tests at human A 1 , A 2A , A 2B , and A 3 adenosine receptor subtypes. Eleven purines showed potent antagonism at A 1 , A 3 , dual A 1 /A 2A , A 1 /A 2B , or A 1 /A 3 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.
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معلومات مُعتمدة: UID/QUI/00686/2020, UID/QUI/ 00686/2018; SFRH/BD/22270/2005; SFRH/BD/85937/2012; SFRH/BPD/ 26106/2005 Fundação para a Ciência e Tecnologia; POCI-01-0145-FEDER-031354 FEDER funds through the Operational Programme for Competitiveness Factors (COMPETE 2020), Programa Operacional de Competitividade e Internacionalização (POCI); PINFRA/22161/2016 Rede Nacional de RMN; ED431C 2022/20 Xunta de Galicia; ERDF European Regional Development Fund
فهرسة مساهمة: Keywords: 2-arylpurine derivatives; G protein-coupled receptors; adenine derivatives; adenosine receptor antagonists; structure-activity relationship
المشرفين على المادة: 0 (Purinergic P1 Receptor Antagonists)
0 (Receptors, Purinergic P1)
JAC85A2161 (Adenine)
0 (Morpholines)
0 (Purines)
تواريخ الأحداث: Date Created: 20240619 Date Completed: 20240619 Latest Revision: 20240718
رمز التحديث: 20240718
مُعرف محوري في PubMed: PMC11173536
DOI: 10.3390/molecules29112543
PMID: 38893418
قاعدة البيانات: MEDLINE
الوصف
تدمد:1420-3049
DOI:10.3390/molecules29112543