Pub. Date : 1992 Nov 27
PMID : 1469686
4 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Following the discovery of a new series of 1-benzyl-4-[2-(N-benzoyl-N-methylamino)ethyl]piperidine (2) derivatives with a potent anti-acetylcholinesterase (anti-AChE) activity, we extended the structure-activity relationships (SAR) to rigid analogues (4) and 1-benzyl-4-[2-(N-benzoyl-N-phenylamino)ethyl]piperidine derivatives (3). | 1-benzyl-4-[2-(n-benzoyl-n-methylamino)ethyl]piperidine | acetylcholinesterase | Rattus norvegicus |
| 2 | Following the discovery of a new series of 1-benzyl-4-[2-(N-benzoyl-N-methylamino)ethyl]piperidine (2) derivatives with a potent anti-acetylcholinesterase (anti-AChE) activity, we extended the structure-activity relationships (SAR) to rigid analogues (4) and 1-benzyl-4-[2-(N-benzoyl-N-phenylamino)ethyl]piperidine derivatives (3). | 1-benzyl-4-[2-(n-benzoyl-n-phenylamino)ethyl]piperidine | acetylcholinesterase | Rattus norvegicus |
| 3 | The rigid analogue containing isoindolone (9) was found to exhibit potent anti-AChE activity comparable to that of 2. | Isoindol-1-one | acetylcholinesterase | Rattus norvegicus |
| 4 | Among the compounds prepared in these series, 1-benzyl-4-[2-[4-(benzoylamino)phthalimido]ethyl]piperidine hydrochloride (19) (IC50 = 1.2 nM) is one of the most potent inhibitors of AChE. | 1-benzyl-4-[2-[4-(benzoylamino)phthalimido]ethyl]piperidine hydrochloride | acetylcholinesterase | Rattus norvegicus |