Kikuchi, H., Okazaki, K., Sekiya, M., Uryu, Y., Ueda, K., Katou, Y., Kurata, S., Oshima, Y. (2011). Synthesis and innate immunosuppressive effect of 1,2-cyclopentanediol derivatives.  Eur. J. Med. Chem. 46(4): 1263--1273.

FBrf0213182

Research paper

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.