152361-07-4Relevant academic research and scientific papers
Indoles which have steroid 5-α reductase inhibitory activity
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, (2008/06/13)
The present invention provides compounds of the formula: STR1 and the pharmaceutically acceptable salts thereof, together with pharmaceutically compositions containing, uses of, processes for the preparation of and intermediates used in the preparation of, such compounds.
The development of non-steroidal dual inhibitors of both human 5α- reductase isozymes
Blagg,Ballard,Cooper,Finn,Johnson,MacIntyre,Maw,Spargo
, p. 1517 - 1522 (2007/10/03)
The design, synthesis and biological properties of homochiral non- steroidal inhibitors of both isozymes of human 5α-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).
