| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374287 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
LASSBio-581 is a N-phenylpiperazine derivative designed for the treatment of schizophrenia. In this study, four strains of filamentous fungi were screened for their capabilities to biotransform LASSBio-581. Cunninghamella echinulata ATCC 9244 was chosen to scale up the biosynthesis of the p-hydroxylated metabolite of LASSBio-581. The chemical structure of the metabolite was confirmed by NMR, LC–MS and X-ray crystallography. Binding studies performed on brain homogenate indicated that the p-hydroxylated metabolite can be considered more selective for dopamine receptors than LASSBio-581, and, therefore, can be used to design new selective dopamine inhibitors.
Graphical abstractThe biosynthesis of the p-hydroxylated metabolite of LASSBio-581 by Cunninghamella echinulata and its pharmacological evaluation is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
