Next Article in Journal
Functional Mitochondria Are Important for the Effect of Resveratrol
Next Article in Special Issue
Carbohydrate-Based Host-Guest Complexation of Hydrophobic Antibiotics for the Enhancement of Antibacterial Activity
Previous Article in Journal
Study on the Alkylation Reactions of N(7)-Unsubstituted 1,3-Diazaoxindoles
Previous Article in Special Issue
Silver Nanoparticles Mediated by Costus afer Leaf Extract: Synthesis, Antibacterial, Antioxidant and Electrochemical Properties
Article Menu
Issue 5 (May) cover image

Export Article

Open AccessArticle
Molecules 2017, 22(5), 841;

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
Received: 13 April 2017 / Revised: 8 May 2017 / Accepted: 15 May 2017 / Published: 20 May 2017
Full-Text   |   PDF [413 KB, uploaded 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

Scheme 1

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).

Share & Cite This Article

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.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics



[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top