| 摘要 |
Phenyl pyridinyl piperazine derivatives of formula (I), their enantiomers and diastereoisomers, acid and base addition salts, are new. Phenyl pyridinyl piperazine derivatives of formula (I), their enantiomers and diastereoisomers, acid and base addition salts. X : C(O) or SO 2; R 1T or NR 3R 4; either R 3, R 4H, 1-6C alkyl, 3-8C cycloalkyl or 3-8C cycloalkyl-1-6C alkyl; or NR 3R 45-8 membered ring (where C is optionally replaced by S, N, O, SO or SO 2) (optionally bridged by a 1-6C alkyl and/or optionally to be substituted by T 1); T 1halo, 3-8C cycloalkyl, 1-6C (polyhalo)alkyl, 1-6C alkoxy, COOH, OH, CN, O, NO 2, NH 2 (optionally substituted by 1-6C alkyl); R 21-6C alkyl, 3-8C cycloalkyl, 3-8C cycloalkyl-1-6C alkyl; and T : aryl e.g. phenyl, naphthyl or biphenyl (all optionally substituted by T 1). An independent claim is included for the preparation of (I). [Image] ACTIVITY : Nootropic; Neuroprotective; Cerebroprotective; Anticonvulsant; Tranquilizer; Anorectic; Analgesic; CNS-Gen.; Antiparkinsonian. MECHANISM OF ACTION : Central histaminergic H3 receptor antagonist. The antagonistic activity of (I) against central histaminergic H3 receptor antagonist was tested. The results showed that (I) exhibited a significant antagonistic activity against central histaminergic H3 receptor antagonist. |
