杨丽敏, 王惠宁. 手性包公藤甲素类似物的制备及其生物活性J. 药学学报, 1998, 33(11): 832-835.
引用本文: 杨丽敏, 王惠宁. 手性包公藤甲素类似物的制备及其生物活性J. 药学学报, 1998, 33(11): 832-835.
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Yang Liming, Wang Huining. THE PREPARATION AND BIOACTIVITIES OF CHIRAL ANALOGS OF BAOGONGTENG AJ. Acta Pharmaceutica Sinica, 1998, 33(11): 832-835.
Citation: Yang Liming, Wang Huining. THE PREPARATION AND BIOACTIVITIES OF CHIRAL ANALOGS OF BAOGONGTENG AJ. Acta Pharmaceutica Sinica, 1998, 33(11): 832-835.
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手性包公藤甲素类似物的制备及其生物活性

THE PREPARATION AND BIOACTIVITIES OF CHIRAL ANALOGS OF BAOGONGTENG A

    摘要
  • 摘要: 用化学拆分技术制备了8个手性包公藤甲素类似物,经兔眼缩瞳或扩瞳试验表明,其中(-)-3α-对甲苯磺酰氧基-6β-乙酰氧基莨菪烷有拟胆碱作用,(+)-3α-苯甲酰氧基-6β-乙酰氧基莨菪烷和(+)-3α-对氯苯甲酰氧基-6β-乙酰氧基莨菪烷有抗胆碱作用。

     

    Abstract: Eight chiral analogs of baogongteng A were prepared from (±)-3α-hydroxy-6β-acetoxytropane by chemical resolution. In myotic or mydriatic tests in rabbits, (-)-3α-paramethyl benzenesulfonyloxy-6β-acetoxytropane showed cholinergic activities, while (+)-3α-benzoyloxy-6β-acetoxytropane and (+)-3α-parachloro benzoyloxy-6β-acetoxytropane showed anticholinergic activities.

     

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