| Autor: |
Jorand-Lebrun C; Merck Serono Geneva Research Center, Bat. B3, 9, chemin des Mines, 1211 Geneva, Switzerland. catherine.jorandlebrun@merckserono.net, Brondyk B, Lin J, Magar S, Murray R, Reddy A, Shroff H, Wands G, Weiser W, Xu Q, McKenna S, Brugger N |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Apr 01; Vol. 17 (7), pp. 2080-5. Date of Electronic Publication: 2006 Dec 22. |
| DOI: |
10.1016/j.bmcl.2006.12.062 |
| Abstrakt: |
In the course of a high throughput screening, a series of pyrazole compounds were identified with luteinizing hormone receptor (LH-R) agonist activity. A focused pyrazole library was produced by solid-phase synthesis and key pyrazole regioisomers were obtained selectively in solution. Evaluation of those compounds in a cAMP assay in CHO cells transfected with h-LH receptor allowed us to propose a structure-activity relationship model for this series and led to the identification of the first low molecular weight molecule with in vitro activity in a Leydig cells assay (ED(50)=1.31 microM) and in vivo in a model of testosterone induction in rats (significant effect at 32 mpk ip). |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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