Academic Journal
Synthesis of 1,2,3-Triazolo[4,5-h]quinolone Derivatives with Novel Anti-Microbial Properties against Metronidazole Resistant Helicobacter pylori
| العنوان: | Synthesis of 1,2,3-Triazolo[4,5-h]quinolone Derivatives with Novel Anti-Microbial Properties against Metronidazole Resistant Helicobacter pylori |
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| المؤلفون: | Mohammad Abu-Sini, Amal Mayyas, Nehaya Al-Karablieh, Rula Darwish, Yusuf Al-Hiari, Talal Aburjai, Shereen Arabiyat, Luay Abu-Qatouseh |
| المصدر: | Molecules, Vol 22, Iss 5, p 841 (2017) |
| بيانات النشر: | MDPI AG, 2017. |
| سنة النشر: | 2017 |
| المجموعة: | LCC:Organic chemistry |
| مصطلحات موضوعية: | H. pylori, triazoloquinolone derivatives, synergism, Organic chemistry, QD241-441 |
| الوصف: | 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. |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 1420-3049 22050841 |
| Relation: | http://www.mdpi.com/1420-3049/22/5/841; https://doaj.org/toc/1420-3049 |
| DOI: | 10.3390/molecules22050841 |
| URL الوصول: | https://doaj.org/article/bbfae146133e4db1bd7a335ffa87aad8 |
| رقم الانضمام: | edsdoj.bbfae146133e4db1bd7a335ffa87aad8 |
| قاعدة البيانات: | Directory of Open Access Journals |
Full Text Finder | تدمد: | 14203049 22050841 |
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| DOI: | 10.3390/molecules22050841 |