Acta Biologica Hungarica
Volume/Issue:
Volume 61: Issue 3
Determination of rat 5α-reductase type 1 isozyme activity and its inhibition by novel steroidal oxazolines
Authors:
M. Szécsi University of Szeged 1st Department of Medicine Korányi fasor 8-10 H-6720 Szeged Hungary

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Dóra Ondré University of Szeged Department of Organic Chemistry Dóm tér 8 H-6720 Szeged Hungary

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I. Tóth University of Szeged 1st Department of Medicine Korányi fasor 8-10 H-6720 Szeged Hungary

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S. Magony University of Szeged 1st Department of Medicine Korányi fasor 8-10 H-6720 Szeged Hungary

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J. Wölfling University of Szeged Department of Organic Chemistry Dóm tér 8 H-6720 Szeged Hungary

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Gy. Schneider University of Szeged Department of Organic Chemistry Dóm tér 8 H-6720 Szeged Hungary

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J. Julesz University of Szeged 1st Department of Medicine Korányi fasor 8-10 H-6720 Szeged Hungary

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Pages:
274–281
Online Publication Date:
19 Aug 2010
Publication Date:
01 Sep 2010
Article Category:
Research Article
DOI:
https://doi.org/10.1556/abiol.61.2010.3.4
Keywords:
5α-reductase inhibitors; exo -heterocyclic steroids; rat liver; finasteride
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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 )-17β-(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.

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Cover Acta Biologica Hungarica
Acta Biologica Hungarica
Print ISSN:
0236-5383
Online ISSN:
1588-256X

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Editor(s)-in-Chief: Elekes, Károly

Editorial Board

    1. Csányi, Vilmos (Göd)
    1. Dudits, Dénes (Szeged)
    1. Falus, András (Budapest)
    1. Fischer, Ernő (Pécs)
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    1. Gulya, Károly (Szeged)
    1. Gulyás, Balázs (Stockholm)
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    1. Heszky, László (Gödöllő)
    1. Hideg, Éva (Szeged)
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    1. Janda, Tibor (Martonvásár)
    1. Kavanaugh, Michael P. (Missoula)
    1. Kása, Péter (Szeged)
    1. Klein, Éva (Stockholm)
    1. Kovács, János (Budapest)
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    1. Nässel, Dick R. (Stockholm)
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    1. Sakharov, Dimitri A. (Moscow)
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    1. Sipiczky, Mátyás (Debrecen)
    1. Szeberényi, József (Pécs)
    1. Székely, György (Debrecen)
    1. Tari, Irma (Szeged)
    1. Vágvölgyi, Csaba (Szeged),
    1. L. Zaborszky (Newark)

 

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Acta Biologica Hungarica
Language English
Size  
Year of
Foundation		 1950
Publication
Programme		 changed title
Volumes
per Year		  
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per Year		  
Founder Magyar Tudományos Akadémia
Founder's
Address		 H-1051 Budapest, Hungary, Széchenyi István tér 9.
Publisher Akadémiai Kiadó
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Address		 H-1117 Budapest, Hungary 1516 Budapest, PO Box 245.
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Publisher		 Chief Executive Officer, Akadémiai Kiadó
ISSN 0236-5383 (Print)
ISSN 1588-256X (Online)

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