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Azabenzthiazole inhibitors of leukotriene A4 hydrolase
Bioorganic & medicinal chemistry letters, 2012-12, Vol.22 (24), p.7504-7511
2012

Details

Autor(en) / Beteiligte
Titel
Azabenzthiazole inhibitors of leukotriene A4 hydrolase
Ist Teil von
  • Bioorganic & medicinal chemistry letters, 2012-12, Vol.22 (24), p.7504-7511
Ort / Verlag
Amsterdam: Elsevier Ltd
Erscheinungsjahr
2012
Link zum Volltext
Quelle
Access via ScienceDirect (Elsevier)
Beschreibungen/Notizen
  • Previously, benzthiazole containing LTA4H inhibitors were discovered that were potent (1–3), but were associated with the potential for a hERG liability. Utilizing medicinal chemistry first principles (e.g., introducing rigidity, lowering cLogD) a new benzthiazole series was designed, congeners of 1–3, which led to compounds 7a, 7c, 12a–d which exhibited LTA4H IC50=3–6nM and hERG Dofetilide Binding IC50=8.9–> >10μM.
Sprache
Englisch
Identifikatoren
ISSN: 0960-894X
eISSN: 1464-3405
DOI: 10.1016/j.bmcl.2012.10.036
Titel-ID: cdi_proquest_miscellaneous_1272719774
Format
–
Schlagworte
Animals, Antiinflammatory, Aza Compounds - chemical synthesis, Aza Compounds - chemistry, Aza Compounds - pharmacology, Benzothiazoles - chemical synthesis, Benzothiazoles - chemistry, Benzothiazoles - pharmacology, Biological and medical sciences, chemistry, Congeners, Dose-Response Relationship, Drug, Drug Design, drug formulations, eicosanoids, enzyme inhibitors, Enzyme Inhibitors - chemical synthesis, Enzyme Inhibitors - chemistry, Enzyme Inhibitors - pharmacology, Epoxide Hydrolases - antagonists & inhibitors, Epoxide Hydrolases - metabolism, ether hydrolases, Ether-A-Go-Go Potassium Channels - antagonists & inhibitors, hERG, heterocyclic compounds, Humans, hydrolase, Leukotriene A4 hydrolase, Leukotrienes, Log D, LTA4H, Medical sciences, Mice, Molecular Structure, Pharmacology. Drug treatments, Structure-Activity Relationship

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