Journal
MENDELEEV COMMUNICATIONS
Volume 31, Issue 4, Pages 501-503Publisher
ELSEVIER
DOI: 10.1016/j.mencom.2021.07.021
Keywords
medium-sized rings; 1; 4; 7-thiadiazecines; 7-oxadiazecines; lactam reduction; dopamine D2 receptor; serotonin receptors; trace amine-associated receptor 1
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Funding
- Russian Science Foundation [19-75-30008]
- Russian Science Foundation [19-75-30008] Funding Source: Russian Science Foundation
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Di(het)areno-fused 1,4,7-(oxa)thiadiazecanes were synthesized via the 'hydrated imidazoline ring expansion' (HIRE) method, with two compounds displaying micromolar agonistic activity towards TAAR1. These compounds are suitable as scaffolds for the design of selective aminergic receptor modulators.
Di(het)areno-fused 1,4,7-(oxa)thiadiazecanes were synthesized by the reduction of the corresponding tenmembered 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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