A. V. Sapegin, A. A. Peshkov, E. V. Kanov, R. R. Gainetdinov, B. Duszyńska, A. J. Bojarski, M. Yu. Krasavin, “Novel medium-sized di(het)areno-fused 1,4,7-(oxa)thiadiazecines as probes for aminergic receptors”, Mendeleev Commun., 31:4 (2021), 501

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Mendeleev Communications, 2021, Volume 31, Issue 4, Pages 501–503
DOI: https://doi.org/10.1016/j.mencom.2021.07.021 (Mi mendc969)

This article is cited in 1 scientific paper (total in 1 paper)

Communications

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

A. V. Sapegin^a, A. A. Peshkov^a, E. V. Kanov^b, R. R. Gainetdinov^b, B. Duszyńska^c, A. J. Bojarski^c, M. Yu. Krasavin^ad

^a Institute of Chemistry, St. Petersburg State University, St. Petersburg, Russian Federation
^b Institute of Translational Biomedicine, St. Petersburg State University, St. Petersburg, Russian Federation
^c Department of Medicinal Chemistry, Institute of Pharmacology, Polish Academy of Sciences, Kraków, Poland
^d Immanuel Kant Baltic Federal University, Kaliningrad, Russian Federation

Full-text PDF (186 kB) Citations (1) Supplementary materials

DOI: https://doi.org/10.1016/j.mencom.2021.07.021

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

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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Document Type: Article

Language: English

*Supplementary materials:*
		Supplementary_data_1.pdf	(2.4 Mb)

Citation: A. V. Sapegin, A. A. Peshkov, E. V. Kanov, R. R. Gainetdinov, B. Duszyńska, A. J. Bojarski, M. Yu. Krasavin, “Novel medium-sized di(het)areno-fused 1,4,7-(oxa)thiadiazecines as probes for aminergic receptors”, Mendeleev Commun., 31:4 (2021), 501–503

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https://www.mathnet.ru/eng/mendc/v31/i4/p501

This publication is cited in the following 1 articles:

Citing articles in Google Scholar: Russian citations, English citations
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