Journal
ARCHIV DER PHARMAZIE
Volume 345, Issue 8, Pages 610-621Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.201200025
Keywords
17 ss HSD2; Disubstituted 1H-1; 2; 4-triazoles; Non-steroidal inhibitor; Osteoporosis; Steroidomimetics
Funding
- Deutsche Forschungsgemeinschaft [HA1315/8-1]
- Alexander von Humboldt Foundation (AvH)
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A series of disubstituted-1H-1,2,4-triazole derivatives was synthesized with the aim of developing new non-steroidal inhibitors of 17 beta-hydroxysteroid dehydrogenase type 2 (17 beta HSD2) a novel and attractive target for the treatment of osteoporosis. 17 beta HSD2 catalyzes the oxidation of the highly active estrogen 17 beta-estradiol (E2) and androgen testosterone (T) into the weak estrone and androstenedione, respectively. Inhibition of this enzyme will locally in the bone lead to an increase in E2 and T levels, two key players in the maintenance of the balance between bone resorption and bone formation. In this study, a new class of 17 beta HSD2 inhibitors with a 1H-1,2,4-triazole scaffold was identified; the three best compounds 8b, 8f, and 13a showed moderate 17 beta HSD2 inhibitory activity and a good selectivity toward 17 beta HSD1. They could be a useful tool to map the unexplored enzyme active site.
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