3,16-Bisquaternary ammonium steroid derivatives as neuromuscular blocking agents: Synthesis and biological evaluation
| Autor: | Xianming Hu, Min Feng, Zhigang Rao, Yuling Xiao, Jianrong Xu, Xianbing Ke, Hao Hu, Peng Liu, Zhe Wu, Xuechuan Hong, Hongzhuan Chen |
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| Rok vydání: | 2015 |
| Předmět: |
Male
Drug media_common.quotation_subject medicine.medical_treatment Clinical Biochemistry Chemistry Techniques Synthetic Pharmacology Biochemistry Steroid Mice Structure-Activity Relationship chemistry.chemical_compound Endocrinology medicine Animals Moiety Ammonium Rocuronium Molecular Biology media_common Biological evaluation Chemistry Organic Chemistry Neuromuscular Blocking Agents In vitro Quaternary Ammonium Compounds Steroids medicine.drug |
| Zdroj: | Steroids. 96:103-114 |
| ISSN: | 0039-128X |
| DOI: | 10.1016/j.steroids.2015.01.008 |
| Popis: | 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 in vitro activities than the commenced drug rocuronium. In addition, structure-activity relationship was unveiled. We found that the intact acetylcholine-like moiety in D-ring was not necessary for maintaining activity but both the acetyl group and the quaternary nitrogen were very essential. |
| Databáze: | OpenAIRE |
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