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Open AccessArticle

Synthesis of 1,2,3-Triazolo[4,5-h]quinolone Derivatives with Novel Anti-Microbial Properties against Metronidazole Resistant Helicobacter pylori

Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman 11733, Jordan
Faculty of Health Sciences, American University of Madaba, Madaba 11821, Jordan
Hamdi Mango Center for Scientific Research, University of Jordan, Amman 11914, Jordan
Faculty of Pharmacy, University of Jordan, Amman 11914, Jordan
Salt College, Al-Balqa Applied University, As-Salt 19117, Jordan
Faculty of Pharmacy, University of Petra, Amman 11914, Jordan
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Molecules 2017, 22(5), 841;
Received: 13 April 2017 / Revised: 8 May 2017 / Accepted: 15 May 2017 / Published: 20 May 2017
Helicobacter pylori infection can lead to gastritis, peptic ulcer, and the development of mucosa associated lymphoid tissue (MALT) lymphoma. Treatment and eradication of H. pylori infection can prevent relapse and accelerate the healing of gastric and duodenal ulcers as well as regression of malignancy. Due to the increasing emergence of antibiotic resistance among clinical isolates of H. pylori, alternative approaches using newly discovered antimicrobial agents in combination with the standard antibiotic regimens for the treatment of H. pylori are of major importance. The purpose of the present study was to investigate the effect of newly synthesized 8-amino 7-substituted fluoroquinolone and their correspondent cyclized triazolo derivatives when either alone or combined with metronidazole against metronidazole-resistant H. pylori. Based on 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 best in vitro effect for compounds 4b and 4c. Fractional inhibitory concentration (FIC) mean values showed synergistic pattern in all compounds of Group 5. In addition, additive activities of some of the tested compounds of Group 4 were observed when combined with metronidazole. In contrast, the tested compounds showed no significant urease inhibition activity. These results support the potential of new fluoroquinolone derivatives to be useful in combination with anti-H. pylori drugs in the management of H. pylori-associated diseases. View Full-Text
Keywords: H. pylori; triazoloquinolone derivatives; synergism H. pylori; triazoloquinolone derivatives; synergism
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Abu-Sini, M.; Mayyas, A.; Al-Karablieh, N.; Darwish, R.; Al-Hiari, Y.; Aburjai, T.; Arabiyat, S.; Abu-Qatouseh, L. Synthesis of 1,2,3-Triazolo[4,5-h]quinolone Derivatives with Novel Anti-Microbial Properties against Metronidazole Resistant Helicobacter pylori. Molecules 2017, 22, 841.

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