Oxetanes as Promising Modules in Drug Discovery

Ring the changes: Introduction of an oxetane ring results in remarkably improved physico‐ and biochemical properties of the underlying scaffold. The oxetane ring confers enhanced solubility, reduces the metabolic degredation, lipophilicity, and amphiphilicity, and modulates the basicity of a nearby...

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Veröffentlicht in:	Angewandte Chemie International Edition 2006-11, Vol.45 (46), p.7736-7739
Hauptverfasser:	Wuitschik, Georg, Rogers-Evans, Mark, Müller, Klaus, Fischer, Holger, Wagner, Björn, Schuler, Franz, Polonchuk, Liudmila, Carreira, Erick M.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biotransformation - drug effects Drug Design Drug Stability Ethers, Cyclic - chemistry Ethers, Cyclic - metabolism Ethers, Cyclic - pharmacology Humans metabolism Mice Microsomes - drug effects Microsomes - metabolism Molecular Structure oxetanes small ring systems synthesis design
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Beschreibung
Zusammenfassung:	Ring the changes: Introduction of an oxetane ring results in remarkably improved physico‐ and biochemical properties of the underlying scaffold. The oxetane ring confers enhanced solubility, reduces the metabolic degredation, lipophilicity, and amphiphilicity, and modulates the basicity of a nearby amine group.
ISSN:	1433-7851 1521-3773
DOI:	10.1002/anie.200602343