| 摘要 |
Imidazole derivs of formula (I) and their acid salts are new. In (I), n is 0-2, A is 1,2,3,4-tetrahydronaphth-6-yl, dur-3-yl (opt. 6-substd. by Cl, Br, I, NO2 or CH3), 1- or 2-naphthyl (opt. substd. by Cl or Br), mesitylyl or R3, R4-phenyl. R3=H, OH, NH2, NO2, acetylamino, phenyl, beta-phenethyl, phenoxy, cyclohexy, phenylthio, benzylthio or 1-6C alkyl or alkylthio, R4 is H or may also be OH if R3=OH, m is O or 1. when m =1, the dotted line has no significance and R and R1 are each H, 1-6C alkyl or phenyl, and X is CO, CHOH, CH2 or CH(OCOR2). R2= phenyl, 1-6C alkyl, or mono- or di- 1-6C alkyl - amino. when m=0, the dotted line is a bond, R=H and X is CH (I) are made, e.g. for m=1, X=CO, by reacting imidazole with aCO. CRR1, (CH2)n halo. (I) are anticonvulsants. The cpd. 1-/(N-imidazolyl)acetyl/-4- cyclohexylbenzene has i.p. and oral LD50 in mice 3 g/kg and 2.1 g/kg. respectively and ED50 against electric shock (0.2 sec. 25 mA/60Hz) of 66 and 92 mg/kg. Compared with known anticonvulsants they have higher therapeutic indices and are more easily soluble in water. |
