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The discovery of novel cyclohexylamide CCR2 antagonists
- Source :
- Bioorganic & Medicinal Chemistry Letters. 21:7496-7501
- Publication Year :
- 2011
- Publisher :
- Elsevier BV, 2011.
-
Abstract
- As a result of further SAR studies on a piperidinyl piperidine scaffold, we report the discovery of compound 44, a potent, orally bioavailable CCR2 antagonist. While having some in vitro hERG activity, this molecule was clean in an in vivo model of QT prolongation. In addition, it showed excellent efficacy when dosed orally in a transgenic murine model of acute inflammation.
- Subjects :
- CCR2
Receptors, CCR2
Transgene
Clinical Biochemistry
hERG
Anti-Inflammatory Agents
Drug Evaluation, Preclinical
Administration, Oral
Pharmaceutical Science
Mice, Transgenic
Inflammation
Pharmacology
Biochemistry
QT interval
Mice
Structure-Activity Relationship
chemistry.chemical_compound
In vivo
Drug Discovery
medicine
Animals
Humans
Molecular Biology
biology
Organic Chemistry
Amides
In vitro
Rats
chemistry
Acute Disease
biology.protein
Molecular Medicine
Piperidine
medicine.symptom
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 21
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....c5df78b7755aa9a1b0fc035055841ee6
- Full Text :
- https://doi.org/10.1016/j.bmcl.2011.09.113