A potent, highly insoluble, GnRH antagonist with a 2-phenyl-4-piperazinylbenzimidazole template and a quinoxaline-2,3-dione pharmacophore was modified to maintain GnRH antagonist activity and improve in vitro pharmaceutical properties. Structural changes to the quinoxaline-2,3-dione portion of the molecule resulted in several structures with improved properties and culminated in the discovery of 6-([4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl] methyl)quinoxaline (WAY-207024). The compound was shown to have excellent pharmacokinetic parameters and lowered rat plasma LH levels after oral administration.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/jm801572m | DOI Listing |
Publication Analysis
Top Keywords
gnrh antagonist
8
discovery 6-{4-[2-4-tert-butylphenyl-1h-benzimidazol-4-yl]piperazin-1-yl}methylquinoxaline
4
6-{4-[2-4-tert-butylphenyl-1h-benzimidazol-4-yl]piperazin-1-yl}methylquinoxaline way-207024
4
way-207024 orally
4
orally active
4
active antagonist
4
antagonist gonadotropin
4
gonadotropin releasing
4
releasing hormone
4
hormone receptor
4
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!