Discovery of halogenated eurypamide B analogues as inhibitors of lipid droplet accumulation in macrophages

Rika Obata; Taichi Ohshiro; Hiroshi Tomoda; Shigeru Nishiyama

doi:10.1016/j.bmcl.2005.06.070

Discovery of halogenated eurypamide B analogues as inhibitors of lipid droplet accumulation in macrophages

Bioorg Med Chem Lett. 2005 Oct 1;15(19):4189-91. doi: 10.1016/j.bmcl.2005.06.070.

Authors

Rika Obata¹, Taichi Ohshiro, Hiroshi Tomoda, Shigeru Nishiyama

Affiliation

¹ Department of Chemistry, Faculty of Science and Technology, Keio University, Hiyoshi 3-14-1, Kohoku-ku, Yokohama 223-8522, Japan.

PMID: 16054812
DOI: 10.1016/j.bmcl.2005.06.070

Abstract

Halogenated cyclic isodityrosine-tripeptides were synthesized as analogues of a marine natural product, eurypamide B. Although the original eurypamides showed no inhibitory activity, the new analogues were found to inhibit lipid droplet accumulation in macrophages with a low micromolar IC50 value.

MeSH terms

Animals
Biological Products / pharmacology*
Halogens
Inhibitory Concentration 50
Lipid Metabolism
Lipids / antagonists & inhibitors*
Macrophages, Peritoneal / drug effects
Macrophages, Peritoneal / metabolism*
Mice
Models, Molecular
Molecular Structure
Oligopeptides / chemical synthesis
Oligopeptides / pharmacology
Peptides, Cyclic / chemical synthesis*
Peptides, Cyclic / pharmacology
Structure-Activity Relationship

Substances

Biological Products
Halogens
Lipids
Oligopeptides
Peptides, Cyclic