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Molecules 2017, 22(1), 71; doi:10.3390/molecules22010071

Synthesis of New Nitrofluoroquinolone Derivatives with Novel Anti-Microbial Properties against Metronidazole Resistant H. pylori

1
Faculty of Pharmacy, University of Petra, 11914 Amman, Jordan
2
Faculty of Pharmacy, University of Jordan,11914 Amman, Jordan
3
Faculty of Pharmacy, Al-Zaytoonah University of Jordan, 11733 Amman, Jordan
4
Faculty of Health Sciences, American University of Madaba, 11821 Madaba, Jordan
*
Author to whom correspondence should be addressed.
Academic Editor: Diego Muñoz-Torrero
Received: 6 November 2016 / Revised: 19 December 2016 / Accepted: 28 December 2016 / Published: 4 January 2017
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [406 KB, uploaded 4 January 2017]   |  

Abstract

One of the major therapeutic approaches to preventing relapse and accelerating the healing of duodenal and gastric ulcers is the eradication of Helicobacter pylori. Due to the emergence of antibiotic resistance among clinical strains of H. pylori, alternative approaches using newly discovered antimicrobial agents in combination with the standard regimens for the treatment of H. pylori are increasingly needed. The purpose of the present study was to investigate the effect of newly synthesized 8-nitroflouroqunolone derivatives when used either alone or when combined with metronidazole against metronidazole-resistant H. pylori. Based on the standard antimicrobial susceptibility testing methods and checkerboard titration assay, all of the tested compounds showed interesting antimicrobial activity against 12 clinical strains of H. pylori, with the best in vitro effect for compound 3c. In addition, synergistic and additive activities of some of the tested compounds were observed when combined with metronidazole. Furthermore, among the tested nitroflouroquinolone derivatives, compound 3b showed significant urease inhibition activity with IC50 of 62.5 µg/mL. These results suggest that 8-nitroflouroquinolone derivatives may have a useful role in combination with anti-H. pylori drugs in the management of H. pylori-associated diseases. View Full-Text
Keywords: nitrofluoroquinolones; H. pylori; urease inhibition nitrofluoroquinolones; H. pylori; urease inhibition
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Abu-Qatouseh, L.; Abu-Sini, M.; Mayyas, A.; Al-Hiari, Y.; Darwish, R.; Aburjai, T. Synthesis of New Nitrofluoroquinolone Derivatives with Novel Anti-Microbial Properties against Metronidazole Resistant H. pylori. Molecules 2017, 22, 71.

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