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Acta Biologica Hungarica

, Volume 61, Issue 3, pp 274–281 | Cite as

Determination of Rat 5α-Reductase Type 1 Isozyme Activity and Its Inhibition by Novel Steroidal Oxazolines

  • M. SzécsiEmail author
  • Dóra Ondré
  • I. Tóth
  • S. Magony
  • J. Wölfling
  • Gy. Schneider
  • J. Julesz
Article
First Online:

Abstract

The 5α-reductase type 1 isozyme is a key enzyme in the metabolism of the androgen steroid hormones and inhibitors of this enzyme represent a new pharmacological treatment for several androgen dependent diseases. We developed a radiosubstrate in vitro incubation method for the determination of 5α-reductase type 1 activity using rat liver microsomes as an enzyme source. With this method we have studied the inhibiting activity of novel (5’S)-17ß-(4,5-dihydrooxazol-5-yl)androst-5-en-3-one compounds containing various derivatized phenyl substituents coupled to the exo-heterocyclic moiety. Tests revealed moderate inhibitory actions compared to finasteride, nevertheless, results provide interesting structure-activity relationship data.

Keywords

5α-reductase inhibitors exo-heterocyclic steroids rat liver finasteride 
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© Akadémiai Kiadó, Budapest 2010

This article is distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made.

Authors and Affiliations

  • M. Szécsi
    • 1
    Email author
  • Dóra Ondré
    • 2
  • I. Tóth
    • 1
  • S. Magony
    • 1
  • J. Wölfling
    • 2
  • Gy. Schneider
    • 2
  • J. Julesz
    • 1
  1. 1.1st Department of MedicineUniversity of SzegedSzegedHungary
  2. 2.Department of Organic ChemistryUniversity of SzegedSzegedHungary

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