School of Chemistry and Physics, University of KwaZulu Natal, Durban 4000, South Africa.
Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
Molecules. 2020 Dec 15;25(24):5941. doi: 10.3390/molecules25245941.
A second generation of 4-aminoquinoline- and 8-aminoquinoline-based tetrazoles and lactams were synthesized via the Staudinger and Ugi multicomponent reactions. These compounds were subsequently evaluated in vitro for their potential antiplasmodium activity against a multidrug-resistant K1 strain and for their antitrypanosomal activity against a cultured STIB900 strain. Several of these compounds (-) displayed good antiplasmodium activities (IC = 0.20-0.62 µM) that were comparable to the reference drugs, while their antitrypanosomal activity was moderate (<20 µM). Compound was 2-fold more active than primaquine and was also the most active (IC = 7.01 µM) against and also exhibited excellent aqueous solubility (>200 µM) at pH 7.
第二代基于 4-氨基喹啉和 8-氨基喹啉的四唑和内酰胺通过 Staudinger 和 Ugi 多组分反应合成。这些化合物随后在体外进行了评估，以研究它们对多药耐药 K1 株的潜在抗疟原虫活性和对 STIB900 株的抗锥虫活性。其中一些化合物（-）表现出良好的抗疟原虫活性（IC = 0.20-0.62 μM），与参考药物相当，而它们的抗锥虫活性则适中（<20 μM）。化合物比伯氨喹更具活性，对和也表现出最活跃的活性（IC = 7.01 μM），并且在 pH 7 时也表现出出色的水溶性（>200 μM）。
