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The development of non-steroidal dual inhibitors of both human 5α-reductase isozymes

✍ Scribed by J. Blagg; S.A. Ballard; K. Cooper; P.W. Finn; P.S. Johnson; F. MacIntyre; G.N. Maw; P.L. Spargo

Publisher: Elsevier Science
Year: 1996
Tongue: English
Weight: 338 KB
Volume: 6
Category: Article
ISSN: 0960-894X
DOI: 10.1016/s0960-894x(96)00261-2

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✦ Synopsis

The design, synthesis and biological properties of homochiral non-steroidal inhibitors of both isozymes of human 5¢t-reductase are described. The o-hydroxy aniline moiety of the initial lead (1) can be replaced by a 3-acyl indole isostere, whilst the minimum energy conformation of the benzyl ether in the potent inhibitor ( 3) is mimicked by the conformationally locked benzodioxolane system in the potent non-steroidal inhibitor (7). Pharmacokinetics and oral efficacy in a rat model of BPH are presented for (3) and ( 7).

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