Structural requirement of tunicamycin V for MraY inhibition

  • Bioorg Med Chem. 2019 Apr 15;27(8):1714-1719. doi: 10.1016/j.bmc.2019.02.035.
Kazuki Yamamoto  1 ,  Akira Katsuyama  2 ,  Satoshi Ichikawa  3
Affiliations
  • 1. Faculty of Pharmaceutical Sciences, Hokkaido University, Kita-12, Nishi-6, Kita-ku, Sapporo 060-0812, Japan.
  • 2. Faculty of Pharmaceutical Sciences, Hokkaido University, Kita-12, Nishi-6, Kita-ku, Sapporo 060-0812, Japan; Center for Research and Education on Drug Discovery, Faculty of Pharmaceutical Sciences, Hokkaido University, Kita-12, Nishi-6, Kita-ku, Sapporo 060-0812, Japan.
  • 3. Faculty of Pharmaceutical Sciences, Hokkaido University, Kita-12, Nishi-6, Kita-ku, Sapporo 060-0812, Japan; Center for Research and Education on Drug Discovery, Faculty of Pharmaceutical Sciences, Hokkaido University, Kita-12, Nishi-6, Kita-ku, Sapporo 060-0812, Japan. Electronic address: [email protected].
PMID: 30850266 DOI: 10.1016/j.bmc.2019.02.035
Abstract

Elucidating a structure-activity relationship study by evaluating a series of truncated analogues is a simple but important and effective tactic in medicinal chemistry based on natural products with a large and complex chemical structure. In this study, a series of truncated analogues of tunicamycin V were designed and synthesized and their MraY inhibitory activity was investigated in order to gain insight into the effect of these moieties on MraY inhibition.

Keywords
Antibacterial; Enzyme inhibitor; Natural products; Nucleoside; Structure-activity relationship.
Products