ArticleACS medicinal chemistry letters2013
Discovery of 3,4-Dihydropyrimidin-2(1H)-ones As a Novel Class of Potent and Selective A2B Adenosine Receptor Antagonists.
Article in ACS medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed.
- Biginelli dihydropyrimidines and their acetylated derivatives as L-/T-type calcium channel blockers: Synthesis, enantioseparation, and molecular modeling studies.Archiv der Pharmazie · 2025Article
- Multicomponent Reaction-Assisted Drug Discovery: A Time- and Cost-Effective Green Approach Speeding Up Identification and Optimization of Anticancer Drugs.International journal of molecular sciences · 2023Review
- Exploring the Effect of Halogenation in a Series of Potent and Selective AJournal of medicinal chemistry · 2023Article
- Exploration of chalcones and related heterocycle compounds as ligands of adenosine receptors: therapeutics development.Molecular diversity · 2022Review
- AJournal for immunotherapy of cancer · 2022Article
- Optimization of 2-Amino-4,6-diarylpyrimidine-5-carbonitriles as Potent and Selective AJournal of medicinal chemistry · 2022Article
- Article
- Identification of V6.51L as a selectivity hotspot in stereoselective AScientific reports · 2021Article
- One Pot Synthesis of Micromolar BACE-1 Inhibitors Based on the Dihydropyrimidinone Scaffold and Their Thia and Imino Analogues.Molecules (Basel, Switzerland) · 2020Article
- Highly Efficient Synthesis of Substituted 3,4-Dihydropyrimidin-2-(1Molecules (Basel, Switzerland) · 2019Article
- Structure-Based Design of Potent and Selective Ligands at the Four Adenosine Receptors.Molecules (Basel, Switzerland) · 2017Article
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Authors and funding
11 authors.
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Abstract
We describe the discovery and optimization of 3,4-dihydropyrimidin-2(1H)-ones as a novel family of (nonxanthine) A2B receptor antagonists that exhibit an unusually high selectivity profile. The Biginelli-based hit optimization process enabled a thoughtful exploration of the structure-activity and structure-selectivity relationships for this chemotype, enabling the identification of ligands that combine structural simplicity with excellent hA2B AdoR affinity and remarkable selectivity profiles.
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