Bioorganic & medicinal chemistry letters, 2012-11, Vol.22 (21), p.6688-6693
2012
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Details
- Autor(en) / Beteiligte
- Titel
- The discovery of CCR3/H1 dual antagonists with reduced hERG risk
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2012-11, Vol.22 (21), p.6688-6693
- Ort / Verlag
- Amsterdam: Elsevier Ltd
- Erscheinungsjahr
- 2012
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- A series of dual CCR3/H1 antagonists based on a bispiperidine scaffold were discovered. Introduction of an acidic group overcame hERG liability. Bioavailability was optimised by modulation of physico-chemical properties and physical form to deliver a compound suitable for clinical evaluation.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2012.08.124Titel-ID: cdi_proquest_miscellaneous_1125233026
- Format
- –
- Schlagworte
- Animals, Antagonist, antagonists, bioavailability, Biological and medical sciences, Chemokine, Drug Discovery, Drug Interactions, Ether-A-Go-Go Potassium Channels - antagonists & inhibitors, hERG, Histamine H1 Antagonists - chemistry, Histamine H1 Antagonists - pharmacokinetics, Indexing in process, Medical sciences, Molecular Structure, Pharmacology. Drug treatments, physical properties, physicochemical properties, Piperidines - chemistry, Rats, Receptors, CCR3 - antagonists & inhibitors, risk, Risk Factors