ArticleBioorganic & medicinal chemistry2004
Structure-activity relationships of thiazole and thiadiazole derivatives as potent and selective human adenosine A3 receptor antagonists.
Article in Bioorganic & medicinal chemistry, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
14 citing papers in PubMed, 126 citations in OpenAlex.
- Selective AACS medicinal chemistry letters · 2022Article
- Different patterns of supra-molecular aggregation in three amides containingActa crystallographica. Section E, Crystallographic communications · 2021Article
- AMedicinal research reviews · 2018Review
- 5-(Thiophen-2-yl)-1,3,4-thiadiazole derivatives: synthesis, molecular docking and in vitro cytotoxicity evaluation as potential anticancer agents.Drug design, development and therapy · 2018Article
- Crystal structures of 2-amino-4,4,7,7-tetra-methyl-4,5,6,7-tetra-hydro-1,3-benzo-thia-zol-3-ium benzoate and 2-amino-4,4,7,7-tetra-methyl-4,5,6,7-tetra-hydro-1,3-benzo-thia-zol-3-ium picrate.Acta crystallographica. Section E, Crystallographic communications · 2017Article
- Polymorphism in the structure ofActa crystallographica. Section E, Crystallographic communications · 2017Article
- Adenosine and its receptors as therapeutic targets: An overview.Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2013Article
- Fragment screening at adenosine-A(3) receptors in living cells using a fluorescence-based binding assay.Chemistry & biology · 2012Article
- Medicinal chemistry of the A3 adenosine receptor: agonists, antagonists, and receptor engineering.Handbook of experimental pharmacology · 2009Review
- Synthesis and characterization of some new tetraaldehyde and tetraketone derivatives and X-ray structure of 1,1'-(4,4'-(2-(1,3-bis(4-acetylphenoxy)propan-2-ylidene)propane-1,3-di-yl)bis(oxy)bis(4,1-phenylene))diethanone.International journal of molecular sciences · 2008Article
- N-(1-Acetyl-r-7,c-9-diphenyl-4,8-dithia-1,2-diaza-spiro-[5.4]dec-2-en-3-yl)acet-amide.Acta crystallographica. Section E, Structure reports online · 2008Article
- Docking studies of agonists and antagonists suggest an activation pathway of the A3 adenosine receptor.Journal of molecular graphics & modelling · 2006Article
- Progress in the pursuit of therapeutic adenosine receptor antagonists.Medicinal research reviews · 2006Review
- Exploring 3D-QSAR of thiazole and thiadiazole derivatives as potent and selective human adenosine A3 receptor antagonists+.Journal of molecular modeling · 2005Article
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
Abstract
4-(4-Methoxyphenyl)-2-aminothiazole and 3-(4-methoxyphenyl)-5-aminothiadiazole derivatives have been synthesized and evaluated as selective antagonists for human adenosine A3 receptors. A methoxy group in the 4-position of the phenyl ring and N-acetyl or propionyl substitutions of the aminothiazole and aminothiadiazole templates displayed great increases of binding affinity and selectivity for human adenosine A3 receptors. The most potent A3 antagonist of the present series, N-[3-(4-methoxy-phenyl)-[1,2,4]thiadiazol-5-yl]-acetamide (39) exhibiting a Ki value of 0.79 nM at human adenosine A3 receptors, showed antagonistic property in a functional assay of cAMP biosynthesis involved in one of the signal transduction pathways of adenosine A3 receptors. Molecular modeling study of conformation search and receptor docking experiments to investigate the dramatic differences of binding affinities between two regioisomers of thiadiazole analogues, (39) and (42), suggested possible binding mechanisms in the binding pockets of adenosine receptors.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.