Naphthalene carboxamides as inhibitors of human cytomegalovirus DNA polymerase

详细信息    查看全文

• 作者：Vaillancourt ; Valerie A. ; Cudahy ; Michele M. ; Staley ; Sandra A. ; Brideau ; Roger J. ; Conrad ; Steven J. ; et. al.
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2000
• 出版时间：September, 2000
• 年：2000
• 卷：10
• 期：18
• 页码：2079-2081
• 全文大小：107 K

文摘

ortho-Hydroxynaphthalene carboxamides have been identified as inhibitors of HCMV DNA polymerase. SAR investigations have demonstrated that both the amide and hydroxy functionalities are required for activity. Substitution on the naphthalene ring has led to inhibitors with submicromolar IC₅₀s against HCMV polymerase. These compounds have been found to be >100-fold selective for inhibition of HCMV polymerase versus human alpha polymerase and display antiviral activity in a cell-based plaque reduction assay.