基于 4-/8-氨基喹啉的内酰胺和四唑的合成及体外抗原生动物评价。
Synthesis and In Vitro Antiprotozoan Evaluation of 4-/8-Aminoquinoline-based Lactams and Tetrazoles.
机构信息
School of Chemistry and Physics, University of KwaZulu Natal, Durban 4000, South Africa.
Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
出版信息
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）。
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