Synthesis and innate immunosuppressive effect of 1,2-cyclopentanediol derivatives

Haruhisa Kikuchi, Kaori Okazaki, Mizuki Sekiya, Yasuyuki Uryu, Kazunori Ueda, Yasuhiro Katou, Shoichiro Kurata, Yoshiteru Oshima

Research output: Contribution to journalArticlepeer-review

10 Citations (Scopus)

Abstract

Innate immunity is the front line of self-defense against infectious microorganisms. In mammals, innate immunity interacts with adaptive immunity and plays a key role in regulating the immune response. Therefore, innate immunity is a good pharmaceutical target for the development of immune regulators. After searching for natural substances that regulate innate immunity using an ex vivo Drosophila culture system, we identified a cyclopentanediol-type compound 1 as an immunosuppressor. In this study, we synthesized and evaluated 1 and its derivatives. Several methylamide- or phenylamide-containing derivatives showed effects that were 20-25 times more potent than those of 1.

Original languageEnglish
Pages (from-to)1263-1273
Number of pages11
JournalEuropean Journal of Medicinal Chemistry
Volume46
Issue number4
DOIs
Publication statusPublished - 2011 Apr

Keywords

  • Cyclopentanediol
  • Drosophila
  • Immunosuppressor
  • Innate immunity
  • TNF-α

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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