Chen Qi, Liu Chong, Bowlin Terry L, Schneller Stewart W
Molette Laboratory for Drug Discovery, Department of Chemistry and Biochemistry, Auburn University, Auburn, AL 36849-5312, United States; Department of Chemistry, Slippery Rock University, Slippery Rock, PA 16057, United States.
Molette Laboratory for Drug Discovery, Department of Chemistry and Biochemistry, Auburn University, Auburn, AL 36849-5312, United States.
Bioorg Med Chem Lett. 2018 May 15;28(9):1456-1458. doi: 10.1016/j.bmcl.2018.03.088. Epub 2018 Mar 31.
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 μM and 7, 7.74 μM) and HCMV (only 7, 0.72 μM). No other activity was found. Neither of the diastereomers was cytotoxic in the assays performed.
据报道，将抗病毒候选药物5'-甲基阿瑞吡坦和5'-高阿瑞吡坦的C-4'侧链结构特征合成结合到一对非对映体的C-4'侧链二羟基化阿瑞吡坦（6和7）中。对这两个靶点进行的广泛抗病毒分析发现，它们对乙肝病毒（6，6.7μM；7，7.74μM）和人巨细胞病毒（仅7，0.72μM）有显著效果。未发现其他活性。在进行的试验中，两种非对映体均无细胞毒性。
