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Long-acting contraceptive agents: Aliphatic and alicyclic carboxylic esters of levonorgestrel
Authors:A. Shafiee  M. Vossoghi  F. Savabi  T.G. Watson  K. Schubert  K. Ponsold  W. Werner  H. Wagner  R. Vlahov  V. Tarpanov  M. Boshkova-Ljapova  B. Milenkov  V. Stoilova  J. Vlahov  G. Snatzke  H. Duddeck
Affiliation:2. Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria;1. Lehrstuhl fur Structurchemie, Ruhr Universitat Bochum, 4630 Bochum 1, (F.D.R.) Bulgaria
Abstract:Esters of levonorgestrel (13β-ethyl-17α-ethynyl-17β-hydroxygon-4-en -3-one) with a variety of aliphatic and alicyclic carboxylic acids have been prepared and characterised. In tests for the suppression of estrus in rats, esters with short-chain aliphatic acids and with cyclobutane-carboxylic acid were considerably more active than the standard, norethisterone enanthate (17α-ethynyl-17β-hydroxyestr-4-en-3-one). Such esters show great promise for development as long-acting progestogens.
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