| Title : Synthesis of 8-phenyl substituted 3-benzazecines with allene moiety, their thermal rearrangement and evaluation as acetylcholinesterase inhibitors - Kobzev_2021_Mol.Divers__ |
| Author(s) : Kobzev MS , Titov AA , Alexandrova EV , Purgatorio R , Catto M , Sorokina EA , Borisova TN , Varlamov AV , Altomare CD , Voskressensky LG |
| Ref : Mol Divers , : , 2021 |
|
Abstract :
Various 4'-R-substituted phenyl azacyclic allenes were synthesized in good yields, and their thermal transformations were studied. For the first time, the obtained rearrangement products-new N-bridged cyclopenta[a]indenes, and the corresponding parent allenes were evaluated as potential inhibitors of acetyl- and butyrylcholinesterase. Among the tested compounds, the allene derivative 2g proved to competitively inhibit human AChE with inhibition constant value (K(i)) in the low micromolar range. |
| PubMedSearch : Kobzev_2021_Mol.Divers__ |
| PubMedID: 33538985 |
Kobzev MS, Titov AA, Alexandrova EV, Purgatorio R, Catto M, Sorokina EA, Borisova TN, Varlamov AV, Altomare CD, Voskressensky LG (2021)
Synthesis of 8-phenyl substituted 3-benzazecines with allene moiety, their thermal rearrangement and evaluation as acetylcholinesterase inhibitors
Mol Divers
:
Kobzev MS, Titov AA, Alexandrova EV, Purgatorio R, Catto M, Sorokina EA, Borisova TN, Varlamov AV, Altomare CD, Voskressensky LG (2021)
Mol Divers
: