SYNTHESIS, CHEMICAL PROPERTIES, AND BIOLOGICAL EVALUATIONS OF SOME TWIN-DRUG TYPE C2-SYMMETRICAL DERIVATIVES

被引:8
作者
Fujisaki, Fumiko [1 ]
Usami, Haruka [1 ]
Nakashima, Saya [1 ]
Nishida, Sho [1 ]
Fujioka, Toshihiro [1 ]
Kashige, Nobuhiro [1 ]
Miake, Fumio [1 ]
Sumoto, Kunihiro [1 ]
机构
[1] Fukuoka Univ, Fac Pharmaceut Sci, Jonan Ku, Fukuoka 8140180, Japan
关键词
Aminoguanidine; Oxazolidinone; Symmetrical Molecule; alpha-Glucosidase Inhibition Activity; Antibacterial Activity; SYMMETRY; MEMBER; ROUTE;
D O I
10.3987/COM-12-12654
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
We describe the synthesis and chemical properties of newly designed C-2-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 alpha-glucosidase inhibition activity (IC50 = 76.3 mu mol/L).
引用
收藏
页码:665 / 675
页数:11
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