前列腺素及其类似物XXIII（1）。15-脱氧-16-羟基-16-甲基前列腺素的合成。C13 - C14反式双键对支气管扩张活性的重要性。
Prostaglandins and congeners XXIII (1). Synthesis of 15-deoxy-16-hydroxy-16-methylprostanglandins. The importance of the C13--C14 trans double bond for bronchodilator activity.
作者信息
Chen S M, Grudzinskas C V, Dessy F
出版信息
Prostaglandins. 1979 May;17(5):707-17. doi: 10.1016/s0090-6980(79)80042-8.
PMID:493558
Abstract
The synthesis and bronchodilator activity in the guinea pig of several 15-deoxy-16-hydroxy-16-methylprostaglandin analogs is described. The E2 (VIa) and E1 (VIb) analogs are potent bronchodilators comparable in activity to the natrual prostaglandins, but possessing a longer duration of effect. Replacement of the C13--C14 trans double bond by a cis double bond or an ethylene linkage causes a substantial diminishment of this activity.
摘要
本文描述了几种15-脱氧-16-羟基-16-甲基前列腺素类似物在豚鼠体内的合成及其支气管扩张活性。E2（VIa）和E1（VIb）类似物是强效支气管扩张剂，其活性与天然前列腺素相当，但作用持续时间更长。将C13 - C14反式双键替换为顺式双键或乙烯键会导致这种活性大幅降低。
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