线粒体呼吸复合体III Qi位点的强效抑制剂。
Potent inhibitors of the Qi site of the mitochondrial respiration complex III.
作者信息
Bolgunas Stephen, Clark David A, Hanna Wayne S, Mauvais Patricia A, Pember Steve O
机构信息
DuPont Agricultural Products, Stine/Haskell Research Center, Post Office Box 30, Newark, Delaware 19714, USA.
出版信息
J Med Chem. 2006 Jul 27;49(15):4762-6. doi: 10.1021/jm060408s.
A series of azole-fused salicylamides were prepared as analogues of antimycin and assayed for activity at complex III of the mitochondrial respiratory chain. The activity of these compounds approached that of antimycin in inhibitory potency and some showed growth reduction of Septoria nodorum in vitro. Compound 8a was shown to bind at the Qi site of complex III by red-shift titration of the bc1 complex.
制备了一系列唑并稠合的水杨酰胺作为抗霉素类似物，并对其在线粒体呼吸链复合物III处的活性进行了测定。这些化合物的活性在抑制效力上接近抗霉素，并且一些化合物在体外显示出对小麦颖枯病菌生长的抑制作用。通过bc1复合物的红移滴定表明化合物8a在线粒体呼吸链复合物III的Qi位点上结合。
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