Optimization of 2-Amino-4,6-diarylpyrimidine-5-carbonitriles as Potent and Selective A₁ Antagonists.

ABSTRACT: We herein document a large collection of 108 2-amino-4,6-disubstituted-pyrimidine derivatives as potent, structurally simple, and highly selective A₁AR ligands. The most attractive ligands were confirmed as antagonists of the canonical cyclic adenosine monophosphate pathway, and some pharmacokinetic parameters were preliminarilly evaluated. The library, built through a reliable and efficient three-component reaction, comprehensively explored the chemical space allowing the identification of the most prominent features of the structure-activity and structure-selectivity relationships around this scaffold. These included the influence on the selectivity profile of the aromatic residues at positions R⁴ and R⁶ of the pyrimidine core but most importantly the pro

SUBMITTER: Val C 

PROVIDER: S-EPMC8842224 | biostudies-literature | 2022 Feb

REPOSITORIES: biostudies-literature