| Title : Design, synthesis, evaluation and QSAR analysis of N(1)-substituted norcymserine derivatives as selective butyrylcholinesterase inhibitors - Takahashi_2010_Bioorg.Med.Chem.Lett_20_1718 |
| Author(s) : Takahashi J , Hijikuro I , Kihara T , Murugesh MG , Fuse S , Kunimoto R , Tsumura Y , Akaike A , Niidome T , Okuno Y , Takahashi T , Sugimoto H |
| Ref : Bioorganic & Medicinal Chemistry Lett , 20 :1718 , 2010 |
|
Abstract :
We synthesized a series of N(1)-substituted norcymserine derivatives 7a-p and evaluated their anti-cholinesterase activities. In vitro evaluation showed that the pyridinylethyl derivatives 7m-o and the piperidinylethyl derivative 7p improved the anti-butyrylcholinesterase activity by approximately threefold compared to N(1)-phenethylnorcymserine (PEC, 2). A quantitative structure-activity relationship (QSAR) study indicated that logS might be a key feature of the improved compounds. |
| PubMedSearch : Takahashi_2010_Bioorg.Med.Chem.Lett_20_1718 |
| PubMedID: 20137934 |
Takahashi J, Hijikuro I, Kihara T, Murugesh MG, Fuse S, Kunimoto R, Tsumura Y, Akaike A, Niidome T, Okuno Y, Takahashi T, Sugimoto H (2010)
Design, synthesis, evaluation and QSAR analysis of N(1)-substituted norcymserine derivatives as selective butyrylcholinesterase inhibitors
Bioorganic & Medicinal Chemistry Lett
20 :1718
Takahashi J, Hijikuro I, Kihara T, Murugesh MG, Fuse S, Kunimoto R, Tsumura Y, Akaike A, Niidome T, Okuno Y, Takahashi T, Sugimoto H (2010)
Bioorganic & Medicinal Chemistry Lett
20 :1718