2. Academic Validation
  3. Importance of lipophilicity for potent anti-herpes simplex virus-1 activity of α-hydroxytropolones

Importance of lipophilicity for potent anti-herpes simplex virus-1 activity of α-hydroxytropolones

  • Medchemcomm. 2019 May 30;10(7):1173-1176. doi: 10.1039/c9md00225a.
Alex J Berkowitz 1 2,  Abaigeal D Franson 3,  Andreu Gazquez Cassals 3,  Katherine A Donald 3,  Alice J Yu 3,  Aswin K Garimallaprabhakaran 1,  Lynda A Morrison 3 4,  Ryan P Murelli 1 2
Affiliations

Affiliations

  • 1 Department of Chemistry , Brooklyn College , The City University of New York , Brooklyn , NY , USA . Email: RPMurelli@brooklyn.cuny.edu.
  • 2 Ph.D. Program in Chemistry , The Graduate Center , The City University of New York , New York , NY , USA.
  • 3 Department of Molecular Microbiology and Immunology , Saint Louis University School of Medicine , St. Louis , MO , USA . Email: lynda.morrison@health.slu.edu.
  • 4 Department of Internal Medicine , Saint Louis University School of Medicine , St. Louis , MO , USA.
PMID: 31391890 DOI: 10.1039/c9md00225a
Abstract

We previously reported that troponoid compounds profoundly inhibit replication of herpes simplex virus (HSV)-1 and HSV-2 in Cell Culture, including acyclovir-resistant mutants. Synthesis of 26 alpha-hydroxylated tropolones (αHTs) led to a preliminary structure-activity relationship highlighting the potency of bi-phenyl side chains. Here, we explore the structure-activity relationship in more detail, with a focus on various biaryl and Other lipophilic molecules. Along with our prior structure-function analysis, we present a refined structure-activity relationship that reveals the importance of the lipophilicity and nature of the side chain for potent anti-HSV-1 activity in cells. We expect this new information will help guide future optimization of αHTs as HSV antivirals.

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