Novel Quinazoline Derivatives as Highly Effective A2A Adenosine Receptor Antagonists.

ABSTRACT: The adenosine A_2A receptor (A_2AR) has been identified as a therapeutic target for treating neurodegenerative diseases and cancer. In recent years, we have highlighted the 2-aminoquinazoline heterocycle as an promising scaffold for designing new A_2AR antagonists, exemplified by 6-bromo-4-(furan-2-yl)quinazolin-2-amine 1 (K_i (hA_2AR) = 20 nM). Here, we report the synthesis of new 2-aminoquinazoline derivatives with substitutions at the C6- and C7-positions, and the introduction of aminoalkyl chains containing tertiary amines at the C2-position to enhance antagonist activity and solubility properties. Compound 5m showed a high affinity for hA_2AR with a K_i value of 5 nM and dem

SUBMITTER: Laversin A 

PROVIDER: S-EPMC11357017 | biostudies-literature | 2024 Aug

REPOSITORIES: biostudies-literature