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New chromene scaffolds for adenosine A(2A) receptors: synthesis, pharmacology and structure-activity relationships.
Areias F, Costa M, Castro M, Brea J, Gregori-Puigjané E, Proença MF, Mestres J, Loza MI. Areias F, et al. Eur J Med Chem. 2012 Aug;54:303-10. doi: 10.1016/j.ejmech.2012.05.009. Epub 2012 May 14. Eur J Med Chem. 2012. PMID: 22677030
In silico screening of a collection of 1584 academic compounds identified a small molecule hit for the human adenosine A(2A) receptor (pK(i) = 6.2) containing a novel chromene scaffold (3a). To explore the structure-activity rel
In silico screening of a collection of 1584 academic compounds identified a small molecule hit for the human adenosine A(2A) …
Coumarins and adenosine receptors: New perceptions in structure-affinity relationships.
Fonseca A, Matos MJ, Vilar S, Kachler S, Klotz KN, Uriarte E, Borges F. Fonseca A, et al. Chem Biol Drug Des. 2018 Jan;91(1):245-256. doi: 10.1111/cbdd.13075. Epub 2017 Sep 4. Chem Biol Drug Des. 2018. PMID: 28734062
Adenosine receptor (AR) subtypes are involved in several physiological and pharmacological processes. ...In this context, our research group focused its investigation into the discovery and development of novel, potent and selective AR ligands based on coumarin s
Adenosine receptor (AR) subtypes are involved in several physiological and pharmacological processes. ...In this context, our
Adenosine Receptor Ligands: Coumarin-Chalcone Hybrids as Modulating Agents on the Activity of hARs.
Vazquez-Rodriguez S, Vilar S, Kachler S, Klotz KN, Uriarte E, Borges F, Matos MJ. Vazquez-Rodriguez S, et al. Molecules. 2020 Sep 19;25(18):4306. doi: 10.3390/molecules25184306. Molecules. 2020. PMID: 32961824 Free PMC article.
Adenosine receptors (ARs) play an important role in neurological and psychiatric disorders such as Alzheimer's disease, Parkinson's disease, epilepsy and schizophrenia. ...Coumarin-chalcone hybrid has been established as a new scaffold su
Adenosine receptors (ARs) play an important role in neurological and psychiatric disorders such as Alzheimer's disease,
In search for new chemical entities as adenosine receptor ligands: development of agents based on benzo-gamma-pyrone skeleton.
Gaspar A, Reis J, Matos MJ, Uriarte E, Borges F. Gaspar A, et al. Eur J Med Chem. 2012 Aug;54:914-8. doi: 10.1016/j.ejmech.2012.05.033. Epub 2012 Jun 1. Eur J Med Chem. 2012. PMID: 22703703
A selected series of chromone carboxamides synthesized in our laboratory were evaluated by radioligand binding studies towards adenosine receptors. All the chromone-3-carboxamides (compounds 8-12) exhibit A(2B) receptor displacement percentage superior to 50% …
A selected series of chromone carboxamides synthesized in our laboratory were evaluated by radioligand binding studies towards adenosine