Determination of rat 5α-reductase type 1 isozyme activity and its inhibition by novel steroidal oxazolines

Szécsi, M. and Ondré, Dóra and Tóth, I. and Magony, S. and Wölfling, J. and Schneider, Gy. and Julesz, J. (2010) Determination of rat 5α-reductase type 1 isozyme activity and its inhibition by novel steroidal oxazolines. Acta Biologica Hungarica, 61 (3). pp. 274-281. ISSN 0236-5383

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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 )-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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