3,16-Bisquaternary ammonium steroid derivatives as neuromuscular blocking agents: synthesis and biological evaluation.
作者： Hao Hu , Zhigang Rao , Min Feng , Zhe Wu , Jianrong Xu
DOI: 10.1016/J.STEROIDS.2015.01.008
关键词:
摘要: Neuromuscular blocking agents (NMBAs) are widely used in surgery to achieve skeleton muscles relaxation under light anesthesia status. In this work, we synthesized a series of 3,16-bisquaternary ammonium steroidal NMBAs. Among them, three compounds exhibited higher vitro activities than the commenced drug rocuronium. addition, structure-activity relationship was unveiled. We found that intact acetylcholine-like moiety D-ring not necessary for maintaining activity but both acetyl group and quaternary nitrogen were very essential.
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