17α-乙基-20α-和-20β-二氢孕酮以及其他17α-乙基取代的孕烷作为潜在的抗孕剂。
17alpha-Ethyl-20alpha-and -20beta-dihydroprogesterones and other 17alpha-ethyl-substituted pregnanes as potential contragestational agents.
作者信息
Hahn D W, Allen G, McGuire J L, Kanojia R M, Ostrowski G
出版信息
J Med Chem. 1975 Nov;18(11):1143-5. doi: 10.1021/jm00245a020.
PMID:170404
Abstract
The 17alpha-ethyl-substituted analogs of the two epimeric 20-dihydroprogesterones, allopregnadedione and pregn-5-ene-3,20-dione, were synthesized and evaluated for their possible oral contragestational (postcoital antifertility) activity in the rat. The compounds, though bound strongly to the progesterone receptor in vitro, were inactive preimplantively at 10 mg/kg and postimplantively at 40 mg/kg in vivo.
摘要
合成了两种差向异构的20-二氢孕酮即别孕烯二酮和孕-5-烯-3,20-二酮的17α-乙基取代类似物，并对其在大鼠中可能的口服抗孕（房事后抗生育）活性进行了评估。这些化合物虽然在体外与孕酮受体结合紧密，但在体内，植入前给予10mg/kg以及植入后给予40mg/kg时均无活性。
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