8-(2-Furyl)adenine derivatives as A2A adenosine receptor ligands
-
Add time:08/04/2019 Source:sciencedirect.com
Selective adenosine receptor modulators are potential tools for numerous therapeutic applications, including cardiovascular, inflammatory, and neurodegenerative diseases. In this work, the synthesis and biological evaluation at the four human adenosine receptor subtypes of a series of 9-substituted 8-(2-furyl)adenine derivatives are reported. Results show that 8-(2-furyl)-9-methyladenine is endowed with high affinity at the A2A subtype. Further modification of this compound with introduction of arylacetyl or arylcarbamoyl groups in N6-position takes to different effects on the A2A affinity and in particular on the selectivity versus the other three adenosine receptor subtypes. A molecular modelling analysis at three different A2A receptor crystal structures provides an interpretation of the obtained biological results.
We also recommend Trading Suppliers and Manufacturers of 8-(2-hydroxypropyl)adenosine (cas 134895-33-3). Pls Click Website Link as below: cas 134895-33-3 suppliers
Prev:Difuran-substituted quinoxalines as a novel class of PI3Kα H1047R mutant inhibitors: Synthesis, biological evaluation and structure-activity relationship
Next:Focused screening to identify new adenosine kinase inhibitors) - 【Back】【Close 】【Print】【Add to favorite 】
- Related Information
- Radiosynthesis and in vivo evaluation of a fluorine-18 labeled pyrazine based radioligand for PET imaging of the adenosine A2B receptor08/13/2019
- In vitro and in vivo antileishmanial properties of a 2-n-propylquinoline hydroxypropyl β-cyclodextrin formulation and pharmacokinetics via intravenous route08/12/2019
- Binding of [3H]MSX-2 (3-(3-hydroxypropyl)-7-methyl-8-(m-methoxystyryl)-1-propargylxanthine) to rat striatal membranes — a new, selective antagonist radioligand for A2A adenosine receptors08/11/2019
- Theacrine: A purine alkaloid from Camellia assamica var. kucha with a hypnotic property via the adenosine system08/10/2019
- New potent A1 adenosine receptor radioligands for positron emission tomography08/09/2019
- Structures of Human A1 and A2A Adenosine Receptors with Xanthines Reveal Determinants of Selectivity08/08/2019
- 8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands08/07/2019
- Reaction of epichlorohydrin with adenosine, 2′-deoxyadenosine and calf thymus DNA: Identification of adducts08/06/2019
- Focused screening to identify new adenosine kinase inhibitors08/05/2019
