Design, synthesis, evaluation and QSAR analysis of N1-substituted norcymserine derivatives as selective butyrylcholinesterase inhibitors
| Autor: | Hachiro Sugimoto, Ryo Kunimoto, Tetsuhiro Niidome, Takeshi Kihara, Akinori Akaike, Yoshinori Tsumura, Jun Takahashi, Modachur G. Murugesh, Yasushi Okuno, Ichiro Hijikuro, Takashi Takahashi, Shinichiro Fuse |
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| Rok vydání: | 2010 |
| Předmět: |
Quantitative structure–activity relationship
Chemistry Stereochemistry Physostigmine Organic Chemistry Clinical Biochemistry Quantitative Structure-Activity Relationship Pharmaceutical Science Biochemistry Neuroprotective Agents Design synthesis Derivative (finance) Butyrylcholinesterase Drug Design Drug Discovery Acetylcholinesterase Humans Molecular Medicine Carbamates Cholinesterase Inhibitors Molecular Biology |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 20:1718-1720 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2010.01.057 |
| Popis: | 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 log S might be a key feature of the improved compounds. |
| Databáze: | OpenAIRE |
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