| 摘要 |
N-(piperidinyl)(phenyl)methyl amide derivatives (I) are new. N-(piperidinyl)(phenyl)methyl amide derivatives of formula (I) and their acid addition salts are new. [Image] R 1H, 1-7C alkyl (optionally fluorinated), 3-7C cycloalkyl, (3-7C)cycloalkyl(1-3C)alkyl, phenyl(1-3C)alkyl (optionally mono- or disubstituted with OMe), 2-4C alkenyl or 2-4C alkynyl; X : H, halo, CF 3, 1-4C alkyl or 1-4C alkoxy; R 2naphthyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, triazinyl, indanyl, indenyl, quinolinyl, isoquinolinyl, quinazolinyl, quinoxalinyl, phtalazinyl, thienyl, furyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, thiazolyl, isoxazolyl, isothiazolyl, thiadiazolyl, oxadiazolyl, triazolyl, benzothienyl, benzofuryl, benzimidazolyl, benzothiazolyl, indolyl, isoindolyl, indazolyl, benzoxazolyl, benzisoxazolyl, benzotriazolyl, benzisothiazolyl, dihydroindolyl, pyrrolopyridinyl, furopyridinyl, thienopyridinyl, imidazopyridinyl, oxazolopyridinyl, thiazolopyridinyl, pyrazolopyridinyl, isoxazolopyridinyl, isothiazolopyridinyl, tetrahydroquinolinyl or tetrahydroisoquinolinyl, all optionally substituted with halo, 1-4C alkyl, 1-4C alkoxy, 1-4C alkylthio or Ar; Ar : phenyl optionally substituted with halo, CF 3, 1-4C alkyl or 1-4C alkoxy. ACTIVITY : Nootropic; Neuroleptic; Tranquilizer; Antidepressant; Antialcoholic; Antimigraine; Relaxant; Analgesic; Antiparkinsonian; Anticonvulsant; Neuroprotective. MECHANISM OF ACTION : Glycine transporter inhibitor. Compounds (I) have IC50 values of 0.01-10 MicroM against glycine uptake by SK-N-MC cells expressing native human glycine transporter glyt1. |
