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Development of 6-benzyl substituted 4-aminocarbonyl-1,4-diazepane-2,5-diones as orally active human chymase inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Jun 15; Vol. 17 (12), pp. 3435-9. Date of Electronic Publication: 2007 Mar 30. - Publication Year :
- 2007
-
Abstract
- A novel series of 6-benzyl substituted 4-aminocarbonyl-1,4-diazepane-2,5-diones was designed, synthesized, and evaluated as human chymase inhibitors. From this series, we identified several compounds which were effective, via oral administration, in a mouse model of chronic dermatitis.
- Subjects :
- Administration, Oral
Animals
Azepines chemical synthesis
Benzyl Compounds chemical synthesis
Binding Sites
Dermatitis pathology
Disease Models, Animal
Humans
Inhibitory Concentration 50
Mice
Models, Chemical
Serine Proteinase Inhibitors chemical synthesis
Serine Proteinase Inhibitors therapeutic use
Structure-Activity Relationship
Azepines pharmacology
Benzyl Compounds pharmacology
Chymases antagonists & inhibitors
Dermatitis drug therapy
Serine Proteinase Inhibitors pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 17
- Issue :
- 12
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 17434735
- Full Text :
- https://doi.org/10.1016/j.bmcl.2007.03.085