Author/Authors :
Fujita، نويسنده , , Daisuke and Ichimaru، نويسنده , , Naoya and Abe، نويسنده , , Masato and Murai، نويسنده , , Masatoshi and Hamada، نويسنده , , Takeshi and Nishioka، نويسنده , , Takaaki and Miyoshi، نويسنده , , Hideto، نويسنده ,
Abstract :
Acetogenin analogs in which the bis-adjacent THF ring was replaced with an enantioselectively synthesized 1,2-cyclopentanediol bis-ether skeleton were synthesized to obtain simplified mimics, and their inhibitory effect on mitochondrial NADH–ubiquinone oxidoreductase (complex I) was examined. The results clearly demonstrate that the 1,2-cyclopentanediol bis-ether motif can substitute for the bis-THF ring while maintaining very potent inhibitory activity at the nanomolar level.
