2. Academic Validation
  3. Structural requirement of tunicamycin V for MraY inhibition

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

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: ichikawa@pharm.hokudai.ac.jp.
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.

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