2. Academic Validation
  3. Naphthalene carboxamides as inhibitors of human cytomegalovirus DNA polymerase

Naphthalene carboxamides as inhibitors of human cytomegalovirus DNA polymerase

  • Bioorg Med Chem Lett. 2000 Sep 18;10(18):2079-81. doi: 10.1016/s0960-894x(00)00402-9.
V A Vaillancourt 1,  M M Cudahy,  S A Staley,  R J Brideau,  S J Conrad,  M L Knechtel,  N L Oien,  J L Wieber,  Y Yagi,  M W Wathen
Affiliations

Affiliation

  • 1 Pharmacia, Kalamazoo, MI 49007, USA. valerie.a.vaillancourt@am.pnu.com
PMID: 10999475 DOI: 10.1016/s0960-894x(00)00402-9
Abstract

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.

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