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Literature DB >> 12937017

Antitrypanosomal activities of fluoroquinolones with pyrrolidinyl substitutions.

Elizabeth Nenortas¹, Tomasz Kulikowicz, Christian Burri, Theresa A Shapiro.

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.

Entities: Chemical Disease Species

Mesh：

Substances：

Year: 2003 PMID： 12937017 PMCID： PMC182618 DOI： 10.1128/AAC.47.9.3015-3017.2003

Source DB: PubMed Journal: Antimicrob Agents Chemother ISSN： 0066-4804 Impact factor: 5.191

12 in total

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6 in total

Review 1. State of the art in African trypanosome drug discovery.

Authors: Robert T Jacobs; Bakela Nare; Margaret A Phillips
Journal: Curr Top Med Chem Date: 2011 Impact factor: 3.295

2. Quinolone Amides as Antitrypanosomal Lead Compounds with In Vivo Activity.

Authors: Georg Hiltensperger; Nina Hecht; Marcel Kaiser; Jens-Christoph Rybak; Alexander Hoerst; Nicole Dannenbauer; Klaus Müller-Buschbaum; Heike Bruhn; Harald Esch; Leane Lehmann; Lorenz Meinel; Ulrike Holzgrabe
Journal: Antimicrob Agents Chemother Date: 2016-07-22 Impact factor: 5.191

3. Topoisomerase II from Human Malaria Parasites: EXPRESSION, PURIFICATION, AND SELECTIVE INHIBITION.

Authors: Devaraja G Mudeppa; Shiva Kumar; Sreekanth Kokkonda; John White; Pradipsinh K Rathod
Journal: J Biol Chem Date: 2015-06-08 Impact factor: 5.157

Review 4. Trypanosomatids topoisomerase re-visited. New structural findings and role in drug discovery.

Authors: Rafael Balaña-Fouce; Raquel Alvarez-Velilla; Christopher Fernández-Prada; Carlos García-Estrada; Rosa M Reguera
Journal: Int J Parasitol Drugs Drug Resist Date: 2014-08-24 Impact factor: 4.077

Review 5. Antiviral, antifungal, and antiparasitic activities of fluoroquinolones optimized for treatment of bacterial infections: a puzzling paradox or a logical consequence of their mode of action?

Authors: A Dalhoff
Journal: Eur J Clin Microbiol Infect Dis Date: 2014-12-17 Impact factor: 3.267

6. Synthesis, Antibacterial Evaluation and QSAR of α-Substituted-N₄-Acetamides of Ciprofloxacin and Norfloxacin.

Authors: Amjad M Qandil; Lorca O Al-Zoubi; Amal G Al-Bakri; Haneen A Amawi; Qosay A Al-Balas; Abdulmalik M Alkatheri; Abdulkareem M Albekairy
Journal: Antibiotics (Basel) Date: 2014-06-25

6 in total