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Identification of a sulfonamide series of CCR2 antagonists
- Source :
- Bioorganicmedicinal chemistry letters. 20(13)
- Publication Year :
- 2010
-
Abstract
- A series of sulfonamide CCR2 antagonists was identified by high-throughput screening. Management of molecular weight and physical properties, in particular moderation of lipophilicity and study of pK(a), yielded highly potent CCR2 antagonists exhibiting good pharmacokinetic properties and improved potency in the presence of human plasma.
- Subjects :
- Stereochemistry
Receptors, CCR2
animal diseases
Clinical Biochemistry
Receptors, CCR1
Pharmaceutical Science
Stereoisomerism
Pharmacology
Biochemistry
Chemical synthesis
Mice
Structure-Activity Relationship
Pharmacokinetics
parasitic diseases
Drug Discovery
Structure–activity relationship
Potency
Animals
Humans
Molecular Biology
chemistry.chemical_classification
Sulfonamides
Dose-Response Relationship, Drug
Molecular Structure
Organic Chemistry
Antagonist
hemic and immune systems
Sulfonamide
High-Throughput Screening Assays
chemistry
Lipophilicity
Molecular Medicine
Subjects
Details
- ISSN :
- 14643405
- Volume :
- 20
- Issue :
- 13
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....64cae2e02cf27bec7e4593b9f7adde93