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Azoloazines as A2a receptor antagonists. Structure--activity relationship

Konstantin Valer'evich Savateev 1
Konstantin Valer'evich Savateev
, 
Evgeny Nartsissovich Ulomsky 1
Evgeny Nartsissovich Ulomsky
, 
Ilya Igorevich Butorin 1
Ilya Igorevich Butorin
, 
Valery Nikolaevich Charushin 1, 2
Valery Nikolaevich Charushin
, 
Vladimir Leonidovich Rusinov 1, 2
Vladimir Leonidovich Rusinov
, 
Oleg Nikolaevich Chupakhin 1, 2
Oleg Nikolaevich Chupakhin
1 Ural Federal University named after the First President of Russia B. N. Yeltsin, Ekaterinburg
2 I. Ya. Postovsky Institute of Organic Synthesis, Ural Branch of Russian Academy of Sciences, Ekaterinburg
10.1070/RCR4792
Published 30 November 2017
Review , RCR4792, Volume 87, Issue 7, 636-669
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Savateev K. V. et al. Azoloazines as A2a receptor antagonists. Structure--activity relationship // Russian Chemical Reviews. 2017. Vol. 87. No. 7. pp. 636-669.
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Savateev K. V., Ulomsky E. N., Butorin I. I., Charushin V. N., Rusinov V. L., Chupakhin O. N. Azoloazines as A2a receptor antagonists. Structure--activity relationship // Russian Chemical Reviews. 2017. Vol. 87. No. 7. pp. 636-669.
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TY - JOUR
DO - 10.1070/RCR4792
UR - https://rcr.colab.ws/publications/10.1070/RCR4792
TI - Azoloazines as A2a receptor antagonists. Structure--activity relationship
T2 - Russian Chemical Reviews
AU - Savateev, Konstantin Valer'evich
AU - Ulomsky, Evgeny Nartsissovich
AU - Butorin, Ilya Igorevich
AU - Charushin, Valery Nikolaevich
AU - Rusinov, Vladimir Leonidovich
AU - Chupakhin, Oleg Nikolaevich
PY - 2017
DA - 2017/11/30
PB - ANO Editorial Board of the journal Uspekhi Khimii
SP - 636-669
IS - 7
VL - 87
ER -
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@article{2017_Savateev,
author = {Konstantin Valer'evich Savateev and Evgeny Nartsissovich Ulomsky and Ilya Igorevich Butorin and Valery Nikolaevich Charushin and Vladimir Leonidovich Rusinov and Oleg Nikolaevich Chupakhin},
title = {Azoloazines as A2a receptor antagonists. Structure--activity relationship},
journal = {Russian Chemical Reviews},
year = {2017},
volume = {87},
publisher = {ANO Editorial Board of the journal Uspekhi Khimii},
month = {Nov},
url = {https://rcr.colab.ws/publications/10.1070/RCR4792},
number = {7},
pages = {636--669},
doi = {10.1070/RCR4792}
}
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Savateev, Konstantin Valer'evich, et al. “Azoloazines as A2a receptor antagonists. Structure--activity relationship.” Russian Chemical Reviews, vol. 87, no. 7, Nov. 2017, pp. 636-669. https://rcr.colab.ws/publications/10.1070/RCR4792.
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Abstract

Non-xanthine inhibitors of the adenosine A2a 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 A2a receptor and selectivity for other types of adenosine receptors A1, A2b, A3 are presented.

The bibliography includes 71 references.

Funders

Ministry of Education and Science of the Russian Federation
4.6351.2017/8.9

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