Anti-Inflammatory Activities of 8-Benzylaminoxanthines Showing High Adenosine A_2A and Dual A₁/A_2A Receptor Affinity.

ABSTRACT: Chronic inflammation plays an important role in the development of neurodegenerative diseases, such as Parkinson's disease (PD). In the present study, we synthesized 25 novel xanthine derivatives with variable substituents at the N1-, N3- and C8-position as adenosine receptor antagonists with potential anti-inflammatory activity. The compounds were investigated in radioligand binding studies at all four human adenosine receptor subtypes, A₁, A_2A, A_2B and A₃. Compounds showing nanomolar A_2A and dual A₁/A_2A affinities were obtained. Three compounds, 19, 22 and 24, were selected for further studies. Docking and molecular dynamics simulation studies indicated binding poses and intera

SUBMITTER: Zaluski M 

PROVIDER: S-EPMC10531311 | biostudies-literature | 2023 Sep

REPOSITORIES: biostudies-literature