Stereoselective biosynthesis of 3′-azido-3′-deoxythymidine 5′-O-β-D-ribopyranoside and in vitro evaluation as potential antileishmanial with in silico ADME prediction

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dc.creatorArruda, Evilanna Lima
dc.creatorNunes, Elaine Sousa
dc.creatorJapiassu, Kamila Bohne
dc.creatorSouza, Paula Letícia de Melo
dc.creatorAraujo, Kelly Carolina Frauzino
dc.creatorOliveira, Valéria de
dc.creatorVinaud, Marina Clare
dc.date.accessioned2025-02-27T12:01:14Z
dc.date.available2025-02-27T12:01:14Z
dc.date.issued2019
dc.description.abstractA stereoselective biosynthesis of a new 3′-azido-3′-deoxythymidine 5′-O-β-D-ribopyranoside (AZT-1) has been achieved from zidovudine (AZT) in PDSM medium, catalyzed by filamentous fungi Cunninghamela echinulata ATCC 9244 (16.6 mg/g, dry weigh/AZT) at 29 °C, 250 rpm and yield of 64.6%. Antileishmanial activity of AZT-1 was evaluated on Leishmania (L.) amazonensis and increased for IC50 25μM, 2.0 × 105 cells/mL−1 at 24 h with the glycosylation, and according to the results of the in silico prediction, without compromising bioavailability and metabolic stability. An MTT assay determined the cytotoxicity to human macrophages with IC50 20 μM that was lower than of AZT. Therefore, for design new antileishmanial drug AZT-1 can be used.
dc.identifier.citationARRUDA, Evilanna L. et al. Stereoselective biosynthesis of 3′-azido-3′-deoxythymidine 5′-O-β-D-ribopyranoside and in vitro evaluation as potential antileishmanial with in silico ADME prediction. Process Biochemistry, Amsterdam, v. 87, p. 232-237, 2019. DOI: 10.1016/j.procbio.2019.08.025. Disponível em: https://www.sciencedirect.com/science/article/pii/S1359511319309699. Acesso em: 21 fev.2025.
dc.identifier.doi10.1016/j.procbio.2019.08.025
dc.identifier.issn1359-5113
dc.identifier.issne- 1873-3298
dc.identifier.urihttps://www.sciencedirect.com/science/article/pii/S1359511319309699
dc.language.isoeng
dc.publisher.countryHolanda
dc.publisher.departmentInstituto de Patologia Tropical e Saúde Pública - IPTSP (RMG)
dc.rightsAcesso Restrito
dc.subjectBiosynthesis
dc.subjectCunninghamella
dc.subjectAZT
dc.subjectGlycosylation
dc.subjectAntileishmanial
dc.titleStereoselective biosynthesis of 3′-azido-3′-deoxythymidine 5′-O-β-D-ribopyranoside and in vitro evaluation as potential antileishmanial with in silico ADME prediction
dc.typeArtigo

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