Antitrypanosomal activities of fluoroquinolones with pyrrolidinyl substitutions.
نویسندگان
چکیده
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.
منابع مشابه
Antitrypanosomal activity of fluoroquinolones.
Six fluoroquinolones presently in clinical use and four investigational tetracyclic fluoroquinolones were tested for in vitro activity against bloodstream-form Trypanosoma brucei brucei. All compounds had measurable activity, but the tetracyclic analogs were most potent, with 50% effective concentrations in the low micromolar range. In general, trypanosomes were more susceptible than L1210 leuk...
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ورودعنوان ژورنال:
- Antimicrobial agents and chemotherapy
دوره 47 9 شماره
صفحات -
تاریخ انتشار 2003