A series of carbo- and heterocyclic alpha-hydroxy amide-derived bradykinin B1 antagonists was prepared and evaluated. A 4,4-difluorocyclohexyl alpha-hydroxy amide was incorporated along with a 2-methyl tetrazole in lieu of an oxadiazole to afford a suitable compound with good pharmacokinetic properties, CNS penetration, and clearance by multiple metabolic pathways.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2008.07.126 | DOI Listing |
Publication Analysis
Top Keywords
alpha-hydroxy amide
8
bradykinin receptor
4
receptor antagonists
4
antagonists alpha-hydroxy
4
amide improved
4
improved metabolism
4
metabolism profile
4
profile series
4
series carbo-
4
carbo- heterocyclic
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!