One step N -glycosylation by filamentous fungi biofilm in bioreactor of a new phosphodiesterase-3 inhibitor tetrazole
| Autor: | Paula L. de Melo Souza, Valéria de Oliveira, Boniek G. Vaz, Francine Pazini, Evilanna Lima Arruda, Luciano M. Lião, Ricardo Menegatti |
|---|---|
| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Glycosylation Clinical Biochemistry Ethyl acetate Tetrazoles Pharmaceutical Science Pyrazole Phosphodiesterase 3 Inhibitors 01 natural sciences Biochemistry Structure-Activity Relationship 03 medical and health sciences chemistry.chemical_compound Bioreactors Drug Discovery Bioreactor Tetrazole Molecular Biology Cunninghamella Cunninghamella echinulata Chromatography Dose-Response Relationship Drug Molecular Structure biology Phosphoric Diester Hydrolases 010405 organic chemistry Organic Chemistry Biofilm biology.organism_classification 0104 chemical sciences 030104 developmental biology chemistry Biofilms Molecular Medicine |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 26:3177-3181 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2016.04.085 |
| Popis: | An efficient and rapid process for N-glycosylation of 5-(1-(3-fluorophenyl)-1H-pyrazol-4-yl)-2H-tetrazole-LQFM 021 (1), a new synthetic derivative of pyrazole with phosphodiesterase-3 (PDE-3) inhibitory action, vasorelaxant activity and low toxicity catalyzed by filamentous fungi biofilm in bioreactor was successfully developed. A maximum N-glycosyl yield of 68% was obtained with Cunninghamella echinulata ATCC 9244 biofilm in bioreactor with conditions of 25mgml(-1) of 1 in PDSM medium at 28°C for 96h. After extraction with ethyl acetate, the derivative was identified by Ultrahigh Resolution Mass Spectrometry and (1)H-(13)C HSQC/HMBC. |
| Databáze: | OpenAIRE |
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