| 摘要 |
<p>2H, 3H-benzimidazo(1,2-b)oxazole derivs. of formula (I) can be used to treat the CNS (where R is 1-4C alkyl, CH2Cl, CH2OH, COOR', CONHR2, CH2NHR2, CH2NR3R4, CH2OAr or CH2OCOCH3; R1 is H, 1-4C alkyl or the equiv. of an alkali or alkaline earth metal; R2 is H, 1-4C alkyl or opt. substd. benzoyl; R3 and R4 together with the N atom to which they are attached from phthalimido or a 5 or 6 membered ring opt. contg. other heteroatoms; and Ar is opt. substd. Ph). (I) are new, except those in which R = Et, CH2Cl or CH2OH. (I) are CNS depressants and have an antireserpin activity e.g. (I; R = N-morpholino methyl) in a dose of 45 mg/kg i.p. doubles the duration of Pentobarbital induced narcosis in mice (50 mg/kg Pentobarbital); 55 mg/kg i.p. reduces the spontaneous motility by 50%; 200 mg/kg completely inhibit reserpin induced prosis in mice 60 min. after administration. (I) are of low toxicity e.g. (I; R = N-morpholinomethyl) has Ld50 iv. mice of 147.5 mg/kg. (I) can be used therapeutically esp. to treat disorders of the general and peripheral nervous system e.g. to treat psychomotoric stimulation, insomnia and depressive conditions. A specifically claimed cpd. is 2-(N-morpholino-methyl)-2H, 3H-benzimidazo (1,2-b) oxazole.</p> |
