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Azvudine

Names

[ CAS No. ]:
1011529-10-4

[ Name ]:
Azvudine

[Synonym ]:
4-Amino-1-[(2R,3S,4R,5R)-5-azido-3-fluoro-4-hydroxy-5-(hydroxymethyl)tetrahydro-2-furanyl]-2(1H)-pyrimidinone

Biological Activity

[Description]:

Azvudine is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). Azvudine inhibits NRTI-resistant viral strains[1].

[Related Catalog]:

Signaling Pathways >> Anti-infection >> HIV
Signaling Pathways >> Anti-infection >> HCV
Research Areas >> Infection
Signaling Pathways >> Anti-infection >> HBV
Signaling Pathways >> Anti-infection >> Reverse Transcriptase

[In Vitro]

Azvudine displays strong inhibition on wild-type HIV-1IIIB and HIV-1RF with an EC50 ranging from 30 to 110 pM. The EC50 values of Azvudine against HIV-1KM018, HIV-1TC-1 and HIV-1WAN T69N are 6.92, 0.34 and 0.45 nM, respectively. Azvudine is sensitive to NRTIs-resistant strain HIV-174V, PIs-resistant strains HIV-1L10R/M46I/L63P/V82T/I84V and HIV-1RF V82F/184V, and FIs-resistant strain pNL4-3 gp41 (36G) V38A/N42T. The EC50 values of Azvudine against these resistant strains are 0.11, 0.14, 0.37 and 0.36 nM respectively[1].

[References]

[1]. Wang RR, et al. Azvudine, a novel nucleoside reverse transcriptase inhibitor showed good drug combination features and better inhibition on drug-resistant strains than lamivudine in vitro. PLoS One. 2014 Aug 21;9(8):e105617.

Chemical & Physical Properties

[ Molecular Formula ]:
C9H11FN6O4

[ Molecular Weight ]:
286.220

[ Exact Mass ]:
286.082581

[ LogP ]:
-0.21


Related Compounds