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Cyclopropylamino acid amide as a pharmacophoric replacement for 2,3-diaminopyridine. Application to the design of novel bradykinin B1 receptor antagonists.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2006 Feb 23; Vol. 49 (4), pp. 1231-4. - Publication Year :
- 2006
-
Abstract
- Antagonism of the bradykinin B1 receptor represents a potential treatment for chronic pain and inflammation. Novel antagonists were designed that display low-nanomolar affinity for the human bradykinin B1 receptor and good bioavailability in the rat.
- Subjects :
- Amides chemistry
Amides pharmacology
Analgesics chemistry
Analgesics pharmacology
Animals
Anti-Inflammatory Agents, Non-Steroidal chemistry
Anti-Inflammatory Agents, Non-Steroidal pharmacology
Biological Availability
Cyclopropanes chemistry
Cyclopropanes pharmacology
Drug Design
Humans
Molecular Conformation
Pyridines chemistry
Pyridines pharmacology
Rats
Stereoisomerism
Structure-Activity Relationship
Amides chemical synthesis
Analgesics chemical synthesis
Anti-Inflammatory Agents, Non-Steroidal chemical synthesis
Bradykinin B1 Receptor Antagonists
Cyclopropanes chemical synthesis
Pyridines chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 0022-2623
- Volume :
- 49
- Issue :
- 4
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 16480259
- Full Text :
- https://doi.org/10.1021/jm0511280