2. Academic Validation
  3. Semisynthesis of salviandulin E analogues and their antitrypanosomal activity

Semisynthesis of salviandulin E analogues and their antitrypanosomal activity

  • Bioorg Med Chem Lett. 2014 Jan 15;24(2):442-6. doi: 10.1016/j.bmcl.2013.12.052.
Yutaka Aoyagi 1,  Koji Fujiwara 2,  Akira Yamazaki 2,  Naoko Sugawara 2,  Reiko Yano 3,  Haruhiko Fukaya 2,  Yukio Hitotsuyanagi 2,  Koichi Takeya 4,  Aki Ishiyama 5,  Masato Iwatsuki 5,  Kazuhiko Otoguro 5,  Haruki Yamada 6,  Satoshi Ōmura 6
Affiliations

Affiliations

  • 1 College of Pharmacy, Kinjo Gakuin University, 2-1723 Omori, Moriyama-ku, Nagoya, Aichi 463-8521, Japan. Electronic address: yutaka@kinjo-u.ac.jp.
  • 2 School of Pharmacy, Tokyo University of Pharmacy & Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan.
  • 3 College of Pharmacy, Kinjo Gakuin University, 2-1723 Omori, Moriyama-ku, Nagoya, Aichi 463-8521, Japan.
  • 4 School of Pharmacy, Tokyo University of Pharmacy & Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan. Electronic address: takeyak@toyaku.ac.jp.
  • 5 Research Center for Tropical Diseases, Kitasato Institute for Life Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8642, Japan.
  • 6 Kitasato Institute for Life Sciences, Graduate School of Infection Control Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8642, Japan.
PMID: 24388808 DOI: 10.1016/j.bmcl.2013.12.052
Abstract

A series of analogues of salviandulin E, a rearranged neoclerodane diterpene originally isolated from Salvia leucantha (Lamiaceae), were prepared and their in vitro activity against Trypanosoma brucei brucei was evaluated with currently used therapeutic drugs as positive controls. One of the 19 compounds prepared and assayed in the present study, butanoyl 3,4-dihydrosalviandulin E analogue was found to be a possible candidate for an antitrypanosomal drug with fairly strong antitrypanosomal activity and lower cytotoxicity.

Keywords

Antitrypanosomal activity; Neoclerodane diterpene; Salvia leucantha; Salviandulin E; Semisynthesis.

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