| Literature DB >> 20363131 |
Francine Pazini1, Ricardo Menegatti, José R Sabino, Carolina H Andrade, Gilda Neves, Stela M K Rates, François Noël, Carlos A M Fraga, Eliezer J Barreiro, Valéria de Oliveira.
Abstract
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. 2010 Elsevier Ltd. All rights reserved.Entities:
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Year: 2010 PMID： 20363131 DOI： 10.1016/j.bmcl.2010.03.034
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823