Journal
MENDELEEV COMMUNICATIONS
Volume 31, Issue 4, Pages 488-489Publisher
ELSEVIER
DOI: 10.1016/j.mencom.2021.07.016
Keywords
trace amine associated receptor 1; decarboxylation; Castagnoli-Cushman reaction; stereoselectivity; hydrogenation; lactam reduction; piperidines; bioluminescence resonance energy transfer
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Funding
- Russian Science Foundation [19-75-30008] Funding Source: Russian Science Foundation
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Rare cis-configured 2,4-disubstituted 1-alkylpyridines were synthesized for potential ligands of TAAR1, but showed no affinity as anticipated. However, these novel, druglike compounds will still be valuable in lead generation pursuits.
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 reaction 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 subsequent lead generation pursuits.
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