Banerjee A K, Broughton B J, Burton T S, Caton M P, Christmas A J, Coffee E C, Crowshaw K, Heazell M A, Stuttle K A, Watkins G L
Prostaglandins. 1978 Oct;16(4):541-54. doi: 10.1016/0090-6980(78)90184-3.
The synthesis and gastrointestinal pharmacology of some 11-deoxyprostaglandin E1 analogues are described with results analysed for selectivity from side effects. 11-Deoxygenation reduced potency relative to PGE2 but, as has been reported for natural PGs, 15- or 16-methyl analogues were more potent than the unsubstituted parent compound in the order 16-methyl greater than 15-methyl greater than 16,16-dimethyl. The results suggest that a complex interaction between C-15 and C-16 in methyl analogues affects their profile of activity, but that none of the modifications studied conferred a substantial potency or selectivity advantage over PGE2.
本文描述了一些11-脱氧前列腺素E1类似物的合成及其胃肠道药理学，并分析了其副作用的选择性结果。相对于PGE2，11-脱氧作用降低了效力，但正如天然前列腺素所报道的那样，15-或16-甲基类似物比未取代的母体化合物更有效，顺序为16-甲基大于15-甲基大于16,16-二甲基。结果表明，甲基类似物中C-15和C-16之间的复杂相互作用影响了它们的活性特征，但所研究的修饰均未赋予比PGE2更大的效力或选择性优势。
