PROSTAGLANDINS AND CONGENERS .22. SYNTHESIS OF 11-SUBSTITUTED DERIVATIVES OF 11-DEOXYPROSTAGLANDINS E1 AND E2 - POTENTIAL BRONCHODILATORS

PROSTAGLANDINS AND CONGENERS .22. SYNTHESIS OF 11-SUBSTITUTED DERIVATIVES OF 11-DEOXYPROSTAGLANDINS E1 AND E2 - POTENTIAL BRONCHODILATORS
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DOI:
10.1021/jm00182a018
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发表时间:
1980-01-01
影响因子:
7.3
通讯作者:
VANHUMBEECK, L
VANHUMBEECK, L
中科院分区:
医学1区
文献类型:
--
作者:
FLOYD, MB;SCHAUB, RE;VANHUMBEECK, L

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本文报道了l-11-deoxy-11.alpha.-[(2-hydroxyethyl)thio]prostaglandin-E_2甲酯(3a)对豚鼠的有趣的支气管扩张活性。还描述了通过对PG[前列腺素]A系列的各种成员进行迈克尔型加成或使用锂铜酸盐共轭加成过程进行全合成来制备3a及其类似物。讨论了本系列中的结构-活性关系。
The interesting bronchodilator activity of l-11-deoxy-11.alpha.-[(2-hydroxyethyl)thio]prostaglandin E2 methyl ester (3a) in guinea pigs is described. The preparation of 3a and its analogs by Michael-type additions to various members of the PG[prostaglandin]A series or by total synthesis using the lithiocuprate conjugate addition process is also described. Structure-activity relationships in this series are discussed.