K. V. Savateev, E. N. Ulomsky, I. I. Butorin, V. N. Charushin, V. L. Rusinov, O. N. Chupakhin, “Azoloazines as <nobr>$\mathrm{A}_{2a}$</nobr> receptor antagonists. Structure–activity relationship”, Usp. Khim., 2018, Volume 87, Issue 7,Pages <nobr>636

This article is cited in 29 papers

Azoloazines as $\mathrm{A}_{2a}$ receptor antagonists. Structure–activity relationship

K. V. Savateev^a, E. N. Ulomsky^a, I. I. Butorin^a, V. N. Charushin^ab, V. L. Rusinov^ab, O. N. Chupakhin^ab

^a Ural Federal University named after the First President of Russia B. N. Yeltsin, Ekaterinburg
^b I. Ya. Postovsky Institute of Organic Synthesis, Ural Branch of Russian Academy of Sciences, Ekaterinburg

Abstract: Non-xanthine inhibitors of the adenosine $\mathrm{A}_{2a}$ receptor of the azoloazine series are good candidates for use as drugs for the treatment of neurodegenerative diseases and sepsis. This review systematizes and summarizes the structure–activity relationships in the series of triazoloazines, including annulated pyrimidines, pyrazines and triazines, as well as their tricyclic fused analogues. The above relationships for such systems are analyzed. The structures of the most efficient functional moieties from the point of view of affinity for the $\mathrm{A}_{2a}$ receptor and selectivity for other types of adenosine receptors ($\mathrm{A}_1$, $\mathrm{A}_{2b}$, $\mathrm{A}_3$) are presented.
The bibliography includes 71 references.

Received: 24.10.2017

DOI: 10.1070/RCR4792