This paper describes the rational design and synthesis of novel inhibitors of human steroid 5a-reductase. Steroidal nitrones were synthesised via an eight-step sequence from epiandrosterone and were tested for activity against type I and II 5a-reductase isozymes. Judicious placement of the nitrone i
Synthesis of 4,17-diazasteroid inhibitors of human 5α-reductase
✍ Scribed by Jacek W. Morzycki; Zenon z.xl;Lotowski; Agnieszka Z. Wilczewska; J. Darren Stuart
- Publisher
- Elsevier Science
- Year
- 1996
- Tongue
- English
- Weight
- 566 KB
- Volume
- 4
- Category
- Article
- ISSN
- 0968-0896
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✦ Synopsis
The synthesis of the 17-aza isomer of finasteride is described. With the side chain amide group of the compound existing in the Z configuration the structure is similar to one of the two favored conformations of finasteride. A series of 4.17-diazasteroids was assayed against the isoenzymes of human 5~-reductase.
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