Institut für Pharmazeutische und Medizinische Chemie, Heinrich Heine Universität, Universitätsstrasse 1, 40225 Düsseldorf, Germany.
J Med Chem. 2011 Oct 13;54(19):6796-802. doi: 10.1021/jm200694q. Epub 2011 Sep 13.
Reverse hydroxamate-based inhibitors of IspC, a key enzyme of the non-mevalonate pathway of isoprenoid biosynthesis and a validated antimalarial target, were synthesized and biologically evaluated. The binding mode of one derivative in complex with EcIspC and a divalent metal ion was clarified by X-ray analysis. Pilot experiments have demonstrated in vivo potential.
基于羟肟酸的 IspC 反向抑制剂的合成与生物学评价，IspC 是异戊烯生物合成非甲羟戊酸途径的关键酶，也是经证实的抗疟靶点。通过 X 射线分析阐明了一种衍生物与 EcIspC 和二价金属离子复合物的结合模式。初步实验证明了其体内潜力。
