Nepveu Francoise, Najahi Ennaji, Valentin Alexis
Universite de Toulouse III, UPS, UMR 152 PHARMA-DEV, 118 Route de Narbonne, F-31062 Toulouse Cedex 9, France.
Curr Top Med Chem. 2014;14(14):1643-52. doi: 10.2174/1568026614666140808121329.
The search for antimalarial compounds continues to be an area of intensive investigation in medicinal chemistry. This review presents the structural variations around the indolone-N-oxide core. From these pharmacomodulation studies, new antiplasmodial agents with various structures have emerged. Most of the molecules generated from reduced forms of the indolone scaffold have led to compounds with antiplasmodial properties. These results confirm the importance of the redox reversibility of the bioreducible N=C bond in these series to obtain antimalarial activities.
寻找抗疟化合物仍然是药物化学中一个深入研究的领域。本综述介绍了吲哚酮 - N - 氧化物核心周围的结构变化。通过这些药效调节研究,出现了各种结构的新型抗疟药。吲哚酮支架还原形式产生的大多数分子都产生了具有抗疟特性的化合物。这些结果证实了这些系列中可生物还原的N = C键的氧化还原可逆性对于获得抗疟活性的重要性。