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异构2-托烷醇的副交感神经阻滞(抗胆碱能)酯。2. 非乙醇酸酯。

Parasympatholytic (anticholinergic) esters of the isomeric 2-tropanols. 2. Non-glycolates.

作者信息

Atkinson E R, McRitchie-Ticknor D D, Harris L S, Archer S, Aceto M D, Pearl J, Luduena F P

出版信息

J Med Chem. 1983 Dec;26(12):1772-5. doi: 10.1021/jm00366a023.

Abstract

The 19 esters in Table I were prepared from (+)-2 alpha-tropanol, (-)-2 beta-tropanol, (+/-)-3-quinuclidinol, and a variety of non-glycolic acids in order to compare their central and peripheral activities with those of the glycolates reported in the previous paper. The results (Table II) showed that esters 6 and 17 were approximately equivalent to one another and to atropine, that 8 was equal in both central and peripheral activity to reference glycolates, that 9 and 19 were less active than 8 but 9 had a substantially reduced central activity, and that 10 and 11 were more active than the methoxy analogue reported earlier.

摘要

制备表I中的19种酯是用(+)-2α-托烷醇、(-)-2β-托烷醇、(±)-3-奎宁环醇和多种非乙醇酸,以便将它们的中枢和外周活性与前一篇论文中报道的乙醇酸酯的活性进行比较。结果(表II)表明,酯6和17彼此大致相当且与阿托品相当,8的中枢和外周活性与参比乙醇酸酯相同,9和19的活性低于8,但9的中枢活性大幅降低,并且10和11比先前报道的甲氧基类似物活性更高。

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