ChemMedChem, 2012-09, Vol.7 (9), p.1546-1550
2012
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Details
- Autor(en) / Beteiligte
- Titel
- Anti-influenza Drug Discovery: Identification of an Orally Bioavailable Quinoline Derivative through Activity- and Property-Guided Lead Optimization
- Ist Teil von
- ChemMedChem, 2012-09, Vol.7 (9), p.1546-1550
- Ort / Verlag
- Weinheim: WILEY-VCH Verlag
- Erscheinungsjahr
- 2012
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- From a high‐throughput screening (HTS) hit with inhibitory activity against virus‐induced cytophathic in the low micromolar range, we have developed a potent anti‐influenza lead through careful optimization without compromising the drug‐like properties of the compound. An orally bioavailable compound was identified as a lead agent with nanomolar activity against influenza, representing a 140‐fold improvement over the initial hit.
- Sprache
- Englisch; Deutsch
- Identifikatoren
- ISSN: 1860-7179eISSN: 1860-7187DOI: 10.1002/cmdc.201200259Titel-ID: cdi_proquest_miscellaneous_1776661685
- Format
- –
- Schlagworte
- Animals, Antiviral Agents - chemistry, Antiviral Agents - pharmacokinetics, Antiviral Agents - pharmacology, Cell Line, Drug Discovery, hit-to-lead optimization, Humans, influenza, Influenza A Virus, H1N1 Subtype - drug effects, Influenza, Human - drug therapy, Male, Orthomyxoviridae Infections - drug therapy, pharmacokinetics, Quinolines - chemistry, Quinolines - pharmacokinetics, Quinolines - pharmacology, Rats, Rats, Sprague-Dawley, Structure-Activity Relationship, structure-activity relationships