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Short Paper | Regular issue | Vol 87, No. 3, 2013, pp.665-675
Published online, 22nd January, 2013
DOI: 10.3987/COM-12-12654
Synthesis, Chemical Properties, and Biological Evaluations of Some Twin-Drug Type C2-Symmetrical Derivatives

Fumiko Fujisaki, Haruka Usami, Saya Nakashima, Sho Nishida, Toshihiro Fujioka, Nobuhiro Kashige, Fumio Miake, and Kunihiro Sumoto*

*Faculty of Pharmaceutical Sciences, Fukuoka University, 8-19-1 Nanakuma, Jonan-ku, Fukuoka 814-0180, Japan

Abstract

We describe the synthesis and chemical properties of newly designed C2-symmetrical twin-drug type aminoguanidines or 4-aminomethyloxazolidinone derivatives (4-7) in which a long chain alkyl group [-(CH2)10-] was used as a linker. Synthesis of some triplet-drug type symmetrical oxazolidinones (8) is also described. Among the tested compounds, the aminoguanidine derivative 4a showed the highest α-glucosidase inhibition activity (IC50 = 76.3 μmol/L).