4-芳基噻吩并[2,3-b]吡啶-2-甲酰胺类是一类新型的抗疟药物。
4-Arylthieno[2,3-]pyridine-2-carboxamides Are a New Class of Antiplasmodial Agents.
机构信息
Institut für Medizinische und Pharmazeutische Chemie, Technische Universität Braunschweig, 38106 Braunschweig, Germany.
Zentrum für Pharmaverfahrenstechnik (PVZ), Technische Universität Braunschweig, Franz-Liszt-Straße 35A, 38106 Braunschweig, Germany.
出版信息
Molecules. 2020 Jul 13;25(14):3187. doi: 10.3390/molecules25143187.
Malaria causes hundreds of thousands of deaths every year, making it one of the most dangerous infectious diseases worldwide. Because the pathogens have developed resistance against most of the established anti-malarial drugs, new antiplasmodial agents are urgently needed. In analogy to similar antiplasmodial ketones, 4-arylthieno[2,3-]pyridine-2-carboxamides were synthesized by Thorpe-Ziegler reactions. In contrast to the related ketones, these carboxamides are only weak inhibitors of the plasmodial enzyme GSK-3 but the compounds nevertheless show strong antiparasitic activity. The most potent representatives inhibit the pathogens with IC values in the two-digit nanomolar range and exhibit high selectivity indices (>100).
疟疾每年导致数十万人死亡，是全球最危险的传染病之一。由于病原体对大多数已确立的抗疟药物产生了耐药性，因此急需新的抗疟药物。受类似的抗疟酮启发，通过 Thorpe-Ziegler 反应合成了 4-芳基噻吩并[2,3-b]吡啶-2-甲酰胺。与相关的酮类化合物不同，这些甲酰胺仅对疟原虫酶 GSK-3 具有较弱的抑制作用，但这些化合物仍具有很强的抗寄生虫活性。最有效的代表物以两位数纳摩尔范围的 IC 值抑制病原体，并表现出高选择性指数（>100）。
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