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Pharmaceutical Chemistry Journal

, Volume 46, Issue 4, pp 203–206 | Cite as

Synthesis and biological activity of synthetic 17α-hydroxyprogesterone derivatives

  • O. A. Zeinalov
  • V. V. Yaderets
  • T. S. Stytsenko
  • M. A. Petrosyan
  • V. A. Andryushina
Article

Gestagenic and contraceptive (in combination with estrogen) activities of megestrol acetate, proligestone, and two esters of mepregenol acetate (butyrate and hemisuccinate) were studied. The absence of a correlation between the gestagenic and contraceptive activity (CA) of the synthetic derivatives of 17α-hydroxyprogesterone was established. Of two compounds (proligestone and megestrol acetate) showing the maximum (100%) CA (in combination with ethynylestradiol), proligestone was practically devoid of gestagenic activity while megestrol acetate was a highly active gestagen. It was confirmed that the gestagenic activities of injected megestrol acetate and mepregenol acetate tended to exceed their peroral activities. Pure estrogen was found to contribute to the CA of the mepregenol esters.

Key words

gestagens contraceptive activity 17α-hydroxyprogesterone derivatives proligestone 

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Copyright information

© Springer Science+Business Media, Inc. 2012

Authors and Affiliations

  • O. A. Zeinalov
    • 1
  • V. V. Yaderets
    • 1
  • T. S. Stytsenko
    • 1
  • M. A. Petrosyan
    • 2
  • V. A. Andryushina
    • 1
  1. 1.Bioengineering Centre, Russian Academy of SciencesMoscowRussia
  2. 2.Research Institute of Obstetrics and GynecologyRussian Academy of Medical SciencesSt. PetersburgRussia

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