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

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Novel medium-sized di(het)areno-fused 1,4,7-(oxa)thiadiazecines as probes for aminergic receptors. / Sapegin, Alexander V.; Peshkov, Anatoly A.; Kanov, Evgeny V.; Gainetdinov, Raul R.; Duszyńska, Beata; Bojarski, Andrzej J.; Krasavin, Mikhail.

в: Mendeleev Communications , Том 31, № 4, 01.07.2021, стр. 501-503.

Результаты исследований: Научные публикации в периодических изданиях › статья › Рецензирование

BibTeX

@article{4c35c1de72794099b0b15b9dd28166e7,

title = "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 {\textquoteleft}hydrated imidazoline ring expansion{\textquoteright} (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.",

keywords = "1,4,7-oxadiazecines, 1,4,7-thiadiazecines, dopamine D receptor, lactam reduction, medium-sized rings, serotonin receptors, trace amine-associated receptor 1",

author = "Sapegin, {Alexander V.} and Peshkov, {Anatoly A.} and Kanov, {Evgeny V.} and Gainetdinov, {Raul R.} and Beata Duszy{\'n}ska and Bojarski, {Andrzej J.} and Mikhail Krasavin",

note = "Publisher Copyright: {\textcopyright} 2021",

year = "2021",

month = jul,

day = "1",

doi = "10.1016/j.mencom.2021.07.021",

language = "English",

volume = "31",

pages = "501--503",

journal = "Mendeleev Communications",

issn = "0959-9436",

publisher = "Elsevier",

number = "4",

}

RIS

TY - JOUR

T1 - Novel medium-sized di(het)areno-fused 1,4,7-(oxa)thiadiazecines as probes for aminergic receptors

AU - Sapegin, Alexander V.

AU - Peshkov, Anatoly A.

AU - Kanov, Evgeny V.

AU - Gainetdinov, Raul R.

AU - Duszyńska, Beata

AU - Bojarski, Andrzej J.

AU - Krasavin, Mikhail

PY - 2021/7/1

Y1 - 2021/7/1

N2 - 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.

AB - 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.

KW - 1,4,7-oxadiazecines

KW - 1,4,7-thiadiazecines

KW - dopamine D receptor

KW - lactam reduction

KW - medium-sized rings

KW - serotonin receptors

KW - trace amine-associated receptor 1

UR - http://www.scopus.com/inward/record.url?scp=85113693004&partnerID=8YFLogxK

U2 - 10.1016/j.mencom.2021.07.021

DO - 10.1016/j.mencom.2021.07.021

M3 - Article

AN - SCOPUS:85113693004

VL - 31

SP - 501

EP - 503

JO - Mendeleev Communications

JF - Mendeleev Communications

SN - 0959-9436

IS - 4

ER -

ID: 85382951