| 摘要 |
Amino acid derivs. of formulae (Ia) and (Ib), and their acid-addn. salts, are new: (where R4 is H, Me, cyclopropylmethyl, di(1-4C alkyl) aminoethyl, methoxymethyl or CH2CH2OH; X is N or CR6; Ra and Rb are H, lower alkyl or CH2OH; R is halogen, NO2 or CF3; R1 is H or lower alkyl; R2 is an acyl gp. derived from a naturally occurring amino acid (in L or DL form if contg. an asymmetric centre); R3 is phenyl, halophenyl or 2-pyridyl), and have sedative, muscle relaxant and anticonvulsant activity, e.g. with an anticonvulsant ED50 of 2-4 mg/kg (i.v., mouse) and an LD50 of 70-120 mg/kg (i.v., mouse) |
