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2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists
- Source :
- Bioorganic & Medicinal Chemistry Letters. 15:1993-1996
- Publication Year :
- 2005
- Publisher :
- Elsevier BV, 2005.
-
Abstract
- We report the discovery and optimization of substituted 2-piperazinecarboxamides as potent and selective agonists of the melanocortin subtype-4 receptor. The 5- and 6-alkylated piperazine compounds exhibit low bioactivation potential as measured by covalent binding in microsome preparations.
- Subjects :
- Agonist
Stereochemistry
medicine.drug_class
Clinical Biochemistry
Pharmaceutical Science
Carboxamide
Biochemistry
Piperazines
Structure-Activity Relationship
chemistry.chemical_compound
Drug Discovery
medicine
Humans
Receptor
Molecular Biology
biology
Chemistry
Organic Chemistry
biology.organism_classification
In vitro
Piperazine
Microsoma
Microsome
Receptor, Melanocortin, Type 4
Molecular Medicine
Melanocortin
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 15
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....44e32b60eac4ad2438147bfe723f3834
- Full Text :
- https://doi.org/10.1016/j.bmcl.2005.02.068