Design and synthesis of N-alkyldeoxynojirimycin derivatives with improved metabolic stability as inhibitors of BVDV and Tacaribe virus.

Yanming Du,Hong Ye,Fang Guo,Lijuan Wang,Tina Gill, Noshena Khan,Andrea Cuconati,Ju-Tao Guo,Timothy M Block,Jinhong Chang,Xiaodong Xu

Bioorganic & Medicinal Chemistry Letters（2013）

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摘要

Novel N-alkyldeoxynojirimycins (NADNJs) based on our previous lead 3 were designed, synthesized and tested in metabolic assays and in virus cultures. NADNJs containing terminal tertiary benzamide, sulfonamide, urea, and oxazolidinone moieties were discovered to have improved metabolic stability compared to 3, while maintaining submicromolar EC50 against BVDV and Tacaribe virus; and low cytotoxicity.

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关键词

N-Alkyldeoxynojirimycin,Sulfonamide,Urea,Oxazolidinone,Metabolic stability,Antiviral,BVDV,Tacaribe

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