类肌钙蛋白。3. N-肌钙蛋白草氨酸酯的合成及抗过敏活性

Troponoids. 3. Synthesis and antiallergy activity of N-troponyloxamic acid esters.

作者信息

Bagli J F, Bogri T, Palameta B, Martel R, Robinson W, Pugsley T, Lippmann W

出版信息

J Med Chem. 1979 Oct;22(10):1186-93. doi: 10.1021/jm00196a008.

DOI:10.1021/jm00196a008

Abstract

A number of oxamic acid derivatives of tropones and tropolones were synthesized and their antianaphylactic activity was determined in passive paw anaphylaxis (PPA). Several of these esters possessed oral activity. A comparison of the effect on the biological activity of the esters and the corresponding acid and its salt is reported. The experiments suggesting a relationship between the activity and the bioavailability of the ester 19 are also described. A study of the fate of ester 19 in serum on oral or intravenous administration to rats and dogs is reported. In vitro results of the effect of the compounds 19, 45, and 45a on the activity of the guinea pig lung and beef heart phosphodiesterase are presented. The various factors that may contribute to the antiallergy activity of compounds of this series are discussed.

摘要

合成了多种卓酚酮和环庚三烯酚酮的草氨酸衍生物，并在被动爪过敏反应（PPA）中测定了它们的抗过敏活性。其中几种酯具有口服活性。报告了对酯、相应的酸及其盐的生物活性影响的比较。还描述了表明酯19的活性与生物利用度之间关系的实验。报告了对大鼠和狗口服或静脉注射酯19后在血清中的代谢情况的研究。给出了化合物19、45和45a对豚鼠肺和牛心磷酸二酯酶活性影响的体外实验结果。讨论了可能有助于该系列化合物抗过敏活性的各种因素。

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