Bioorganic & medicinal chemistry letters, 2010-07, Vol.20 (13), p.3961-3964
2010
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Details
- Autor(en) / Beteiligte
- Titel
- Identification of a sulfonamide series of CCR2 antagonists
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2010-07, Vol.20 (13), p.3961-3964
- Ort / Verlag
- Amsterdam: Elsevier Ltd
- Erscheinungsjahr
- 2010
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- 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 p K a, yielded highly potent CCR2 antagonists exhibiting good pharmacokinetic properties and improved potency in the presence of human plasma.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2010.04.142Titel-ID: cdi_proquest_miscellaneous_754869619
- Format
- –
- Schlagworte
- Animals, Biological and medical sciences, Bones, joints and connective tissue. Antiinflammatory agents, CCR2 antagonists, Dose-Response Relationship, Drug, High-Throughput Screening Assays, Humans, Medical sciences, Mice, Molecular Structure, p Ka, Pharmacology. Drug treatments, Receptors, CCR1 - antagonists & inhibitors, Receptors, CCR2 - antagonists & inhibitors, Stereoisomerism, Structure-Activity Relationship, Sulfonamides, Sulfonamides - chemistry, Sulfonamides - pharmacology