title: Semisynthesis of salviandulin E analogues and their antitrypanosomal activity.
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.
authors.affiliation: College of Pharmacy, Kinjo Gakuin University, 2-1723 Omori, Moriyama-ku, Nagoya, Aichi 463-8521, Japan. Electronic address: yutaka@kinjo-u.ac.jp.
authors.forename: Yutaka
authors.initials: Y
authors.lastname: Aoyagi
authors.affiliation: School of Pharmacy, Tokyo University of Pharmacy & Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan.
authors.forename: Koji
authors.initials: K
authors.lastname: Fujiwara
authors.affiliation: School of Pharmacy, Tokyo University of Pharmacy & Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan.
authors.forename: Akira
authors.initials: A
authors.lastname: Yamazaki
authors.affiliation: School of Pharmacy, Tokyo University of Pharmacy & Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan.
authors.forename: Naoko
authors.initials: N
authors.lastname: Sugawara
authors.affiliation: College of Pharmacy, Kinjo Gakuin University, 2-1723 Omori, Moriyama-ku, Nagoya, Aichi 463-8521, Japan.
authors.forename: Reiko
authors.initials: R
authors.lastname: Yano
authors.affiliation: School of Pharmacy, Tokyo University of Pharmacy & Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan.
authors.forename: Haruhiko
authors.initials: H
authors.lastname: Fukaya
authors.affiliation: School of Pharmacy, Tokyo University of Pharmacy & Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan.
authors.forename: Yukio
authors.initials: Y
authors.lastname: Hitotsuyanagi
authors.affiliation: School of Pharmacy, Tokyo University of Pharmacy & Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan. Electronic address: takeyak@toyaku.ac.jp.
authors.forename: Koichi
authors.initials: K
authors.lastname: Takeya
authors.affiliation: Research Center for Tropical Diseases, Kitasato Institute for Life Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8642, Japan.
authors.forename: Aki
authors.initials: A
authors.lastname: Ishiyama
authors.affiliation: Research Center for Tropical Diseases, Kitasato Institute for Life Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8642, Japan.
authors.forename: Masato
authors.initials: M
authors.lastname: Iwatsuki
authors.affiliation: Research Center for Tropical Diseases, Kitasato Institute for Life Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8642, Japan.
authors.forename: Kazuhiko
authors.initials: K
authors.lastname: Otoguro
authors.affiliation: Kitasato Institute for Life Sciences, Graduate School of Infection Control Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8642, Japan.
authors.forename: Haruki
authors.initials: H
authors.lastname: Yamada
authors.affiliation: Kitasato Institute for Life Sciences, Graduate School of Infection Control Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8642, Japan.
authors.forename: Satoshi
authors.initials: S
authors.lastname: Ōmura
mesh_terms: D018360:Crystallography, X-Ray; D006801:Humans; D010936:Plant Extracts / Q000138:chemical synthesis* / Q000494:pharmacology*; D027544:Salvia; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D014346:Trypanosoma brucei brucei / Q000187:drug effects* / Q000502:physiology
chemical_list: D010936:Plant Extracts; D014344:Trypanocidal Agents
keywords: Antitrypanosomal activity; Neoclerodane diterpene; Salvia leucantha; Salviandulin E; Semisynthesis