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Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 2
- Source :
- Bioorganicmedicinal chemistry letters. 16(18)
- Publication Year :
- 2006
-
Abstract
- The design, synthesis, and SAR of a series of retro bis-aminopyrrolidine ureas are described. Compounds from this series exhibited considerable binding affinity (Ki = 1 nM) and functional activity at MCH-R1, acceptable CYP2D6 inhibition, and good rat brain exposure.
- Subjects :
- Pyrrolidines
Melanin-concentrating hormone
medicine.drug_class
Stereochemistry
Clinical Biochemistry
Pharmaceutical Science
Carboxamide
Biochemistry
Chemical synthesis
chemistry.chemical_compound
Inhibitory Concentration 50
Structure-Activity Relationship
Drug Discovery
medicine
Structure–activity relationship
Animals
Urea
Receptors, Somatostatin
skin and connective tissue diseases
Receptor
Molecular Biology
biology
Molecular Structure
Organic Chemistry
Small molecule
Melanin-concentrating hormone receptor
Rats
chemistry
Enzyme inhibitor
biology.protein
Molecular Medicine
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 16
- Issue :
- 18
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....5c331fb020772417ea9042e850f1d81a