STRUCTURE-ACTIVITY RELATIONSHIP STUDY OF KNOWN INHIBITORS OF THE ENZYME 5-ALPHA-REDUCTASE (5AR)

Authors
AHMED S DENISON S
Citation
S. Ahmed et S. Denison, STRUCTURE-ACTIVITY RELATIONSHIP STUDY OF KNOWN INHIBITORS OF THE ENZYME 5-ALPHA-REDUCTASE (5AR), Bioorganic & medicinal chemistry letters, 8(5), 1998, pp. 409-414
Citations number
8
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
5
Year of publication
1998
Pages
409 - 414
Database
ISI
SICI code
0960-894X(1998)8:5<409:SRSOKI>2.0.ZU;2-R
Abstract
Preliminary results of a modelling study of both steroidal and non-ste roidal inhibitors of 5 alpha-reductase (5AR) are described in order to elucidate the essential structural requirements needed for the design of novel non-steroidal inhibitors. The study suggests that : (i) ther e is a requirement for groups to mimic the C(3)=O of the steroid subst rate A-ring; (ii) the area of the active site about the C(17)-OH posit ion of the substrate does not appear to possess hydrogen bonding group s and is unrestricted. (C) 1998 Elsevier Science Ltd. All rights reser ved.