具有吡咯烷基取代的氟喹诺酮类药物的抗锥虫活性。
Antitrypanosomal activities of fluoroquinolones with pyrrolidinyl substitutions.
作者信息
Nenortas Elizabeth, Kulikowicz Tomasz, Burri Christian, Shapiro Theresa A
机构信息
Departments of Medicine and of Pharmacology and Molecular Sciences, The Johns Hopkins University, Baltimore, Maryland 21205, USA.
出版信息
Antimicrob Agents Chemother. 2003 Sep;47(9):3015-7. doi: 10.1128/AAC.47.9.3015-3017.2003.
Abstract
Fluoroquinolones with pyrrolidinyl substitutions were tested against Trypanosoma brucei and mammalian cells. Bulky substituents at C-7 or a 1-2-bridging thiazolidine ring increased antitrypanosomal activity and selective toxicity. These compounds trap protein-DNA complexes and inhibit nucleic acid biosynthesis in trypanosomes, characteristics of topoisomerase II inhibition.
摘要
对带有吡咯烷基取代基的氟喹诺酮类药物进行了抗布氏锥虫和哺乳动物细胞的测试。C-7位的庞大取代基或1,2-桥连噻唑烷环增强了抗锥虫活性和选择性毒性。这些化合物捕获蛋白质-DNA复合物并抑制锥虫中的核酸生物合成，这是拓扑异构酶II抑制的特征。
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