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Molecules 2017, 22(5), 841; doi:10.3390/molecules22050841

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

1
Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman 11733, Jordan
2
Faculty of Health Sciences, American University of Madaba, Madaba 11821, Jordan
3
Hamdi Mango Center for Scientific Research, University of Jordan, Amman 11914, Jordan
4
Faculty of Pharmacy, University of Jordan, Amman 11914, Jordan
5
Salt College, Al-Balqa Applied University, As-Salt 19117, Jordan
6
Faculty of Pharmacy, University of Petra, Amman 11914, Jordan
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 13 April 2017 / Revised: 8 May 2017 / Accepted: 15 May 2017 / Published: 20 May 2017
View Full-Text   |   Download PDF [413 KB, uploaded 20 May 2017]   |  

Abstract

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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MDPI and ACS Style

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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