| 摘要 |
<p>N-(2-Aza-bicyclo[2.2.1]-hex-1-yl)-aryl-methyl-heterobenzamide derivatives (I) and their base or acid addition salts are new. N-(2-Aza-bicyclo[2.2.1]-hex-1-yl)-aryl-methyl-heterobenzamide derivatives of formula (I) and their base or acid addition salts are new. R : H, (1-6C) alkyl or (3-7C)-cycloalkyl optionally substituted by one or more groups comprising halo, (3-7C)-cycloalkyl, (1-6C)alkyl, (1-6C)alkoxy, or OH; R 1>a phenyl or naphthyl (both optionally substituted by one or more substituents of halo, 1-6C alkyl, 1-6C alkoxy, halo-1-6C-alkyl, hydroxy, halo-(1-6C)alkoxy, (1-6C)alkyl-thio, (1-6C)alkyl-SO, or (1-6C)alkyl-SO 2); Het : a heteroaryl group; and R 2>one or more substituents comprising H, halo, halo-(1-6C) alkyl, (1-6C)alkyl, (3-7C)cycloalkyl, (3-7C)-cycloalkyl-(1-3C) alkyl, (1-6C) alkoxy, benzyl, (1-6C)alkyl-thio, (1-6C) alkyl-SO, or (1-6C) alkyl-SO 2. Independent claims are included for: (1) the preparation of (I); (2) C-(2-aza-bicyclo[2.1.1]hex-1-yl)-methylamine compounds of formula (II); and (3) heterocyclic ketone compounds of formula (III). Y 1>a leaving group or Cl. [Image] [Image] ACTIVITY : Nootropic; Neuroleptic; Neuroprotective; Cerebroprotective; Tranquilizer; Antidepressant; Antimanic; Antiaddictive; Antialcoholic; Endocrine-Gen.; Eating-Disorders-Gen.; Antimigraine; Analgesic; Hypnotic. MECHANISM OF ACTION : Glycine transporter 1 (glyt1) inhibitor. The ability of (I) to inhibit glyt1 was tested in SK-N-MC cells (human neuroepithelial cells). The result showed that N-[(2-aza-bicyclo[2.1.1]hex-1-yl)-phenylmethyl]-(3-chloro-4-trifluoromethyl)-pyridine-2-carboxamide exhibited an IC 50value of 0.11 mu M.</p> |
