Grupo de Química Orgánica de Productos Naturales (QOPN), Facultad de Ciencias Exactas y Naturales, Instituto de Química, Universidad de Antioquia, Medellín, Colombia.
PECET-Facultad de Medicina, Universidad de Antioquia, Medellín, Colombia.
Arch Pharm (Weinheim). 2020 Dec;353(12):e2000157. doi: 10.1002/ardp.202000157. Epub 2020 Aug 17.
Chalcones are a group of natural products with many recognized biological activities, including antiparasitic activity. Although a lot of chalcones have been synthetized and assayed against parasites, the number of structural features known to be involved in this biological property is small. Thus, in the present study, 21 chalcones were synthesized to determine the effect of substituents in the A and B rings on the activity against Leishmania braziliensis, Trypanosoma cruzi, and Plasmodium falciparum. The compounds were active against L. braziliensis in a structure-dependent manner. Only one compound was very active against T. cruzi, but none of them had a significant antiplasmodial activity. The electron-donating substituents in ring B and the hydrogen bonds at C-2' with carbonyl affect the antiparasitic activity.
查耳酮是一组具有多种已被认可的生物活性的天然产物，包括抗寄生虫活性。尽管已经合成了许多查耳酮并对寄生虫进行了检测，但已知与这种生物特性相关的结构特征数量较少。因此，在本研究中，合成了 21 种查耳酮，以确定 A 环和 B 环上取代基对巴西利什曼原虫、克氏锥虫和恶性疟原虫活性的影响。这些化合物对 L. braziliensis 的活性具有结构依赖性。只有一种化合物对 T. cruzi 非常有效，但它们都没有显著的抗疟原虫活性。B 环上的供电子取代基和 C-2'与羰基的氢键影响抗寄生虫活性。
