Pellegata R, Pinza M, Pifferi G, Gaiti A, Mozzi R, Tirillini B, Porcellati G
Farmaco Sci. 1981 Oct;36(10):845-55.
The synthesis of new N-substituted 4-hydroxy (III) and 4-acyloxy- or 4-alkoxy-2-pyrrolidinones (IV), as analogues of oxiracetam (III c), is reported. For this purpose, a convenient procedure for N-alkylation of the base-labile 4-hydroxy-2-pyrrolidinones (II a, c, d) was developed. Compounds (III) and (IV) were examined on phospholipid synthesis in brain microsomal membranes of rats, both in vivo and in vivo-in vitro, and on protein synthesis in brain slices. Results showed that only oxiracetam (III c), and to a lesser extent piracetam, are active both on phospholipid and brain protein synthesis.
据报道，合成了新型N-取代的4-羟基（III）以及4-酰氧基或4-烷氧基-2-吡咯烷酮（IV），作为奥拉西坦（III c）的类似物。为此，开发了一种用于对碱不稳定的4-羟基-2-吡咯烷酮（II a、c、d）进行N-烷基化的简便方法。对化合物（III）和（IV）在大鼠脑微粒体膜磷脂合成方面进行了体内和体内-体外研究，并对脑切片中的蛋白质合成进行了研究。结果表明，只有奥拉西坦（III c）以及在较小程度上的吡拉西坦，对磷脂和脑蛋白质合成均有活性。
