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Novel medium-sized di(het)areno-fused 1,4,7-(oxa)thiadiazecines as probes for aminergic receptors

Alexander Vladimirovich Sapegin 1
Alexander Vladimirovich Sapegin
, 
Anatoly Andreevich Peshkov 1
Anatoly Andreevich Peshkov
, 
Evgeny Victorovich Kanov 2
Evgeny Victorovich Kanov
, 
Raul Radikovich Gainetdinov 2
Raul Radikovich Gainetdinov
, 
Beata Duszyńska 3
Beata Duszyńska
, 
Andrzej J Bojarski 3
Andrzej J Bojarski
, 
Mikhail Yur'evich Krasavin 1, 4
Mikhail Yur'evich Krasavin
10.1016/j.mencom.2021.07.021
Published 2021-07-07
Communication , Volume 31, Issue 4, 501-503
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Sapegin A. V. et al. Novel medium-sized di(het)areno-fused 1,4,7-(oxa)thiadiazecines as probes for aminergic receptors // Mendeleev Communications. 2021. Vol. 31. No. 4. pp. 501-503.
GOST all authors (up to 50) Copy
Sapegin A. V., Peshkov A. A., Kanov E. V., Gainetdinov R. R., Duszyńska B., Bojarski A. J., Krasavin M. Y. Novel medium-sized di(het)areno-fused 1,4,7-(oxa)thiadiazecines as probes for aminergic receptors // Mendeleev Communications. 2021. Vol. 31. No. 4. pp. 501-503.
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TY - JOUR
DO - 10.1016/j.mencom.2021.07.021
UR - https://mendcomm.colab.ws/publications/10.1016/j.mencom.2021.07.021
TI - Novel medium-sized di(het)areno-fused 1,4,7-(oxa)thiadiazecines as probes for aminergic receptors
T2 - Mendeleev Communications
AU - Sapegin, Alexander Vladimirovich
AU - Peshkov, Anatoly Andreevich
AU - Kanov, Evgeny Victorovich
AU - Gainetdinov, Raul Radikovich
AU - Duszyńska, Beata
AU - Bojarski, Andrzej J
AU - Krasavin, Mikhail Yur'evich
PY - 2021
DA - 2021/07/07
PB - Mendeleev Communications
SP - 501-503
IS - 4
VL - 31
ER -
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@article{2021_Sapegin,
author = {Alexander Vladimirovich Sapegin and Anatoly Andreevich Peshkov and Evgeny Victorovich Kanov and Raul Radikovich Gainetdinov and Beata Duszyńska and Andrzej J Bojarski and Mikhail Yur'evich Krasavin},
title = {Novel medium-sized di(het)areno-fused 1,4,7-(oxa)thiadiazecines as probes for aminergic receptors},
journal = {Mendeleev Communications},
year = {2021},
volume = {31},
publisher = {Mendeleev Communications},
month = {Jul},
url = {https://mendcomm.colab.ws/publications/10.1016/j.mencom.2021.07.021},
number = {4},
pages = {501--503},
doi = {10.1016/j.mencom.2021.07.021}
}
MLA
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Sapegin, Alexander Vladimirovich, et al. “Novel medium-sized di(het)areno-fused 1,4,7-(oxa)thiadiazecines as probes for aminergic receptors.” Mendeleev Communications, vol. 31, no. 4, Jul. 2021, pp. 501-503. https://mendcomm.colab.ws/publications/10.1016/j.mencom.2021.07.021.

Abstract

Di(het)areno-fused 1,4,7-(oxa)thiadiazecanes were synthesized by the reduction of the corresponding ten-membered lactams obtained, in turn, via the ‘hydrated imidazoline ring expansion’ (HIRE) methodology. Two of them displayed micromolar agonistic activity towards trace amine-associated receptor 1 (TAAR1) and no affinity towards a panel of dopamine (D2) and serotonin (5-HT1A, 5-HT2A and 5-HT7) receptors. These findings validate compounds of this chemotype as scaffolds for the design of selective aminergic receptor modulators.

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