Design and synthesis of novel triazine derivatives as antimalarial agents

  • Bioorg Med Chem Lett. 2025 Apr 1:118:130091. doi: 10.1016/j.bmcl.2024.130091.
Yuko Asamitsu  1 ,  Aki Ishiyama  2 ,  Yui Iwamae  3 ,  Rina Nagao  3 ,  Rei Hokari  2 ,  Masato Iwatsuki  2 ,  Kazuhiko Otoguro  2 ,  Masaaki Sawa  3
Affiliations
  • 1. Carna Biosciences, Inc., 1-5-5 Minatojima-Minamimachi, Chuo-ku, Kobe, Hyogo 650-0047, Japan. Electronic address: [email protected].
  • 2. Graduate School of Infection Control Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan.
  • 3. Carna Biosciences, Inc., 1-5-5 Minatojima-Minamimachi, Chuo-ku, Kobe, Hyogo 650-0047, Japan.
PMID: 39736278 DOI: 10.1016/j.bmcl.2024.130091
Abstract

In a previous study, we reported that nilotinib, a Bcr-Abl tyrosine kinase inhibitor, possesses moderate antimalarial activity against PfK1 and PfFCR3. As a part of our efforts to develop novel antimalarial agents, a series of novel triazine analogs was identified as potent antimalarial agents via structure modification of nilotinib. Compound 15a showed strong antimalarial activities against PfK1 and PfFCR3 with IC50 values of 0.28 and 0.29 µM, respectively.

Keywords
1,3,5-Triazine; Antimalarial activity; Nilotinib; Structure-activity relationship.
Products