Rare cis-configured 2,4-disubstituted 1-alkylpiperidines: synthesized and tested against trace-amine-associated receptor 1 (TAAR1)

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Rare cis-configured 2,4-disubstituted 1-alkylpiperidines: synthesized and tested against trace-amine-associated receptor 1 (TAAR1). / Levashova, Ekaterina ; Firsov, Andrey ; Bakulina, Olga ; Peshkov, Anatoly ; Kanov, Evgeny ; Gainetdinov, Raul R.; Krasavin, Mikhail.

в: Mendeleev Communications , Том 31, № 4, 27.08.2021, стр. 488-489.

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

BibTeX

@article{0272e2b1e3ca4b41a2bda1d96a77f7c9,

title = "Rare cis-configured 2,4-disubstituted 1-alkylpiperidines: synthesized and tested against trace-amine-associated receptor 1 (TAAR1)",

abstract = "Rare cis-configured 2,4-disubstituted 1-alkylpyridines were envisioned as ligands for trace amine associated receptor 1 (TAAR1). They were synthesized in diastereomerically pure form with the decarboxylative Castagnoli–Cushman reac-tion followed by two reduction events. Despite showing no affinity to TAAR1 as was anticipated, these novel, druglike and CNS-focused compounds will be of much utility in sub-sequent lead generation pursuits.",

keywords = "bioluminescence resonance energy transfer, Castagnoli–Cushman reaction, decarboxylation, hydrogenation, lactam reduction, piperidines, stereoselectivity, trace amine associated receptor 1",

author = "Ekaterina Levashova and Andrey Firsov and Olga Bakulina and Anatoly Peshkov and Evgeny Kanov and Gainetdinov, {Raul R.} and Mikhail Krasavin",

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

year = "2021",

month = aug,

day = "27",

doi = "10.1016/j.mencom.2021.07.016",

language = "English",

volume = "31",

pages = "488--489",

journal = "Mendeleev Communications",

issn = "0959-9436",

publisher = "Elsevier",

number = "4",

}

RIS

TY - JOUR

T1 - Rare cis-configured 2,4-disubstituted 1-alkylpiperidines: synthesized and tested against trace-amine-associated receptor 1 (TAAR1)

AU - Levashova, Ekaterina

AU - Firsov, Andrey

AU - Bakulina, Olga

AU - Peshkov, Anatoly

AU - Kanov, Evgeny

AU - Gainetdinov, Raul R.

AU - Krasavin, Mikhail

PY - 2021/8/27

Y1 - 2021/8/27

N2 - Rare cis-configured 2,4-disubstituted 1-alkylpyridines were envisioned as ligands for trace amine associated receptor 1 (TAAR1). They were synthesized in diastereomerically pure form with the decarboxylative Castagnoli–Cushman reac-tion followed by two reduction events. Despite showing no affinity to TAAR1 as was anticipated, these novel, druglike and CNS-focused compounds will be of much utility in sub-sequent lead generation pursuits.

AB - Rare cis-configured 2,4-disubstituted 1-alkylpyridines were envisioned as ligands for trace amine associated receptor 1 (TAAR1). They were synthesized in diastereomerically pure form with the decarboxylative Castagnoli–Cushman reac-tion followed by two reduction events. Despite showing no affinity to TAAR1 as was anticipated, these novel, druglike and CNS-focused compounds will be of much utility in sub-sequent lead generation pursuits.

KW - bioluminescence resonance energy transfer

KW - Castagnoli–Cushman reaction

KW - decarboxylation

KW - hydrogenation

KW - lactam reduction

KW - piperidines

KW - stereoselectivity

KW - trace amine associated receptor 1

UR - http://www.scopus.com/inward/record.url?scp=85113165988&partnerID=8YFLogxK

UR - https://www.mendeley.com/catalogue/af624bc1-a354-3b70-9f12-ae93e8427caa/

U2 - 10.1016/j.mencom.2021.07.016

DO - 10.1016/j.mencom.2021.07.016

M3 - Article

AN - SCOPUS:85113165988

VL - 31

SP - 488

EP - 489

JO - Mendeleev Communications

JF - Mendeleev Communications

SN - 0959-9436

IS - 4

ER -

ID: 85025424