期刊
CHEMICAL BIOLOGY & DRUG DESIGN
卷 86, 期 4, 页码 663-673出版社
WILEY-BLACKWELL
DOI: 10.1111/cbdd.12534
关键词
chemical biology; drug design; drug discovery
资金
- NIH [AI098091, 9RO1 GM 110569-06]
The emergence of drug-resistant strains of influenza virus makes exploring new classes of inhibitors that target universally conserved viral targets a highly important goal. The influenza A viral genome is made up of eight single-stranded RNA-negative segments. The RNA promoter, consisting of the conserved sequences at the 3 and 5 end of each RNA genomic segment, is universally conserved among influenza A virus strains and in all segments. Previously, we reported on the identification and NMR structure of DPQ (6,7-dimethoxy-2-(1-piperazinyl)-4-quinazolinamine) (compound 1) in complex with the RNA promoter. Here, we report on additional screening and SAR studies with compound 1, including exvivo anti-influenza activity assays, resulted in improved cellular activity against influenza A virus in the micromolar range.
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