Author: Ross D. Overacker; Somdev Banerjee; George F. Neuhaus; Selena Milicevic Sephton; Alexander Herrmann; James A. Strother; Ruth Brack-Werner; Paul R. Blakemore; Sandra Loesgen
Title: Biological Evaluation of Molecules of the azaBINOL Class as Antiviral Agents: Specific Inhibition of HIV-1 RNase H Activity by 7-Isopropoxy-8-(naphth-1-yl)quinoline Document date: 2019_1_23
ID: m2zw8eq4_7
Snippet: Next we used the EASY-HIT full viral infection assay system 35 to test all six isopropyl ether 161 and carbamate azaBINOL derivatives against fully-infectious, replication competent HIV-1LAI 162 (Table 2 ). The quinol-type 2´-deoxy-8-azaBINOL ether B#24 continued to exhibit low 163 micromolar antiviral activity in the EASY-HIT assay system in accordance with results obtained 164 from the HIVpp assay. Surprisingly, the naphthol-type 2-deoxy-8-aza.....
Document: Next we used the EASY-HIT full viral infection assay system 35 to test all six isopropyl ether 161 and carbamate azaBINOL derivatives against fully-infectious, replication competent HIV-1LAI 162 (Table 2 ). The quinol-type 2´-deoxy-8-azaBINOL ether B#24 continued to exhibit low 163 micromolar antiviral activity in the EASY-HIT assay system in accordance with results obtained 164 from the HIVpp assay. Surprisingly, the naphthol-type 2-deoxy-8-azaBINOL ether B#59 165 exhibited increased antiviral activity. The deoxy-8-azaBINOL carbamate derivatives B#43 and 166 B#60 gave similar high micromolar viral neutralization but also displayed comparable 167 cytotoxicity. The analogous 2-deoxy-8,8´-diazaBINOL compounds, B#57 and B#58, showed no 168 antiviral activity or cytotoxicity at concentrations tested up to 200 µM. 169
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