Synthesis of oxytocin analogues with replacement of sulfur by carbon gives potent antagonists with increased stability

JL Stymiest, BF Mitchell, S Wong…

文献索引：Stymiest, Jake L.; Mitchell, Bryan F.; Wong, Susan; Vederas, John C. Journal of Organic Chemistry, 2005 , vol. 70, # 20 p. 7799 - 7809

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被引用次数: 95

摘要

The neuropeptide oxytocin 1 controls mammary and uterine smooth muscle contraction. Atosiban 2, an oxytocin antagonist, is used for prevention of preterm labor and premature birth. However, the metabolic lifetimes of such peptide drugs are short because of in vivo degradation. Facile production of oxytocin analogues with varying ring sizes wherein sulfur is replaced by carbon (methylene or methine) could be achieved by standard solid-phase ...