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4,5-Dihydropyridazin-3-one derivatives as histamine H3 receptor inverse agonists
- Source :
- Bioorganic & Medicinal Chemistry Letters. 22:194-198
- Publication Year :
- 2012
- Publisher :
- Elsevier BV, 2012.
-
Abstract
- H3R structure–activity relationships for a new class of 4,5-dihydropyridazin-3-one H3R antagonists/inverse agonists are disclosed. Modification of the 4,5-dihydropyridazinone moiety to block in vivo metabolism identified 4,4-dimethyl-6-{4-[3-((R)-2-methyl-pyrrolidin-1-yl)-propoxy]-phenyl}-4,5-dihydro-2H-pyridazin-3-one 22 as a lead candidate demonstrating potent in vivo functional H3R antagonism in the rat dipsogenia model and robust wake promoting activity in the rat EEG/EMG model.
Details
- ISSN :
- 0960894X
- Volume :
- 22
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi...........14e53aafbb7fd56b1ad3f76f26be3953