New kelatorphan-related inhibitors of enkephalin metabolism: improved antinociceptive properties

…, BP Roques, MC Fournie-Zaluski

文献索引：Xie; Soleilhac; Schmidt; Peyroux; Roques; Fournie-Zaluski Journal of Medicinal Chemistry, 1989 , vol. 32, # 7 p. 1497 - 1503

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被引用次数: 42

摘要

Results Chemistry. The various inhibitors were synthesized by using a strategy similar to that previously described for the preparation of kelatorphan and analogues, consisting of two main steps with benzylidenesuccinic acid as the initial precursor (Figure 1). This compound was chosen in order to prevent isomerization between the a and/3 positions observed with the saturated analogue, caused by the nonregioselective opening of the succinimide ...