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10-氧杂-11-脱氧前列腺素E1和10-去甲-9,11-断前列腺素F1及其衍生物的合成与生物学评价

Synthesis and biological evaluation of 10-oxa-11-deoxyprostaglandin E1 and 10-nor-9,11-secoprostaglandin F1 and their derivatives.

作者信息

Carroll F I, Hauser F M, Huffman R C, Coleman M C

出版信息

J Med Chem. 1978 Apr;21(4):321-5. doi: 10.1021/jm00202a001.

Abstract

Three 10-oxa-11-deoxyprostaglandin E1 and two 10-nor-9,11-secoprostaglandin F1 analogues were prepared. The compounds were evaluated for pregnancy interruptions, oxytocin-like activity (uterine strip), and antiprostaglandin activity. One of the 10-nor-9,11-secoprostaglandin F1 analogues displayed activity as a PGE2 antagonist in the gerbil colon smooth muscle preparation.

摘要

制备了三种10-氧杂-11-脱氧前列腺素E1和两种10-去甲-9,11-断前列腺素F1类似物。对这些化合物进行了妊娠中断、催产素样活性(子宫条)和抗前列腺素活性的评估。其中一种10-去甲-9,11-断前列腺素F1类似物在沙鼠结肠平滑肌制备中表现出作为PGE2拮抗剂的活性。

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