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One step N-glycosylation by filamentous fungi biofilm in bioreactor of a new phosphodiesterase-3 inhibitor tetrazole.
de Melo Souza, Paula L; Arruda, Evilanna L; Pazini, Francine; Menegatti, Ricardo; Vaz, Boniek G; Lião, Luciano M; de Oliveira, Valéria.
Affiliation
  • de Melo Souza PL; Laboratório de Bioconversão, Instituto de Química, Universidade Federal de Goiás, P.O. Box 131, Goiânia, GO, Brazil.
  • Arruda EL; Laboratório de Bioconversão, Instituto de Química, Universidade Federal de Goiás, P.O. Box 131, Goiânia, GO, Brazil.
  • Pazini F; Laboratório de Química Farmacêutica, Faculdade de Farmácia, Instituto de Química, Universidade Federal de Goiás, P.O. Box 131, Goiânia, GO, Brazil.
  • Menegatti R; Laboratório de Química Farmacêutica, Faculdade de Farmácia, Instituto de Química, Universidade Federal de Goiás, P.O. Box 131, Goiânia, GO, Brazil.
  • Vaz BG; Laboratório de Cromatografia e Espectrometria de Massas, Instituto de Química, Universidade Federal de Goiás, P.O. Box 131, Goiânia, GO, Brazil.
  • Lião LM; Laboratório de Ressonância Magnética Nuclear, Instituto de Química, Universidade Federal de Goiás, P.O. Box 131, Goiânia, GO, Brazil.
  • de Oliveira V; Laboratório de Bioconversão, Instituto de Química, Universidade Federal de Goiás, P.O. Box 131, Goiânia, GO, Brazil. Electronic address: valeriaoliveira@ufg.br.
Bioorg Med Chem Lett ; 26(13): 3177-3181, 2016 07 01.
Article in En | MEDLINE | ID: mdl-27209234
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.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Tetrazoles / Phosphoric Diester Hydrolases / Biofilms / Bioreactors / Cunninghamella / Phosphodiesterase 3 Inhibitors Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2016 Document type: Article Affiliation country: Brazil Country of publication: United kingdom
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Tetrazoles / Phosphoric Diester Hydrolases / Biofilms / Bioreactors / Cunninghamella / Phosphodiesterase 3 Inhibitors Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2016 Document type: Article Affiliation country: Brazil Country of publication: United kingdom