5′-Hydroxy-5′-homoaristeromycin: Synthesis and antiviral properties

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:28

Article

Chen, Qi^1,2  Liu, Chong¹  Bowlin, Terry L.³  Schneller, Stewart W.¹ 

[1] Auburn Univ, Dept Chem & Biochem, Molette Lab Drug Discovery, Auburn, AL 36849 USA

[2] Slippery Rock Univ, Dept Chem, Slippery Rock, PA 16057 USA

[3] Microbiotix Inc, One Innovat Dr, Worcester, MA 01605 USA

关键词: Carbocyclic nucleosides;    C-4 ' aristeromycin derivatives;    Hepatitis B;    Cytomegalovirus;   

DOI  :  10.1016/j.bmcl.2018.03.088

来源: Elsevier

【 摘 要 】

Synthetically combining the C-4' side-chain structural features of the antiviral candidates 5'-methylaristeromycin and 5'-homoaristeromycin into a diastereomeric pair of C-4' side-chain dihydroxylated aristeromycins (6 and 7) is reported. Broad antiviral analyses of the both targets found promising effects towards HBV (6, 6.7 mu M and 7, 7.74 mu M) and HCMV (only 7, 0.72 mu M). No other activity was found. Neither of the diastereomers was cytotoxic in the assays performed. (C) 2018 Elsevier Ltd. All rights reserved.

【 授权许可】

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