Faculty of Pharmacy, Takasaki University of Health and Welfare.
Department of Molecular and Cellular Parasitology, Graduate School of Health Sciences, Gunma University.
Chem Pharm Bull (Tokyo). 2021;69(12):1195-1199. doi: 10.1248/cpb.c21-00732.
A series of quinone derivatives with a variety of side chains were synthesized. These synthetic quinone compounds were evaluated for in vitro antitrypanosomal activity against trypomastigotes and amastigotes of Trypanosoma cruzi, the causative agent of Chagas disease. Measurement of solubility of quinones and their ability to permeate cell membranes were assessed to address their possible use as oral drugs. Some synthesized compounds exhibited potent antitrypanosomal activity. However, most compounds with a promising activity showed poor solubility that did not seem suitable for oral usage. Meanwhile, compound 5a, an N-tert-butoxycarbonylpiperidine derivative, exhibited good antitrypanosomal activity, ability to permeate membranes, and good solubility.
合成了一系列具有不同侧链的醌衍生物。这些合成的醌类化合物被评估了对引起恰加斯病的克氏锥虫的游离体和滋养体的体外抗锥虫活性。测量了醌的溶解度及其穿透细胞膜的能力，以探讨它们作为口服药物的可能性。一些合成的化合物表现出很强的抗锥虫活性。然而，大多数具有良好活性的化合物的溶解度较差，似乎不适合口服使用。同时，N-叔丁氧羰基哌啶衍生物 5a 表现出良好的抗锥虫活性、膜穿透能力和良好的溶解性。
