Abu-Qatouseh Luay, Abu-Sini Mohammad, Mayyas Amal, Al-Hiari Yusuf, Darwish Rula, Aburjai Talal
Faculty of Pharmacy, University of Petra, 11914 Amman, Jordan.
Faculty of Pharmacy, University of Jordan,11914 Amman, Jordan.
Molecules. 2017 Jan 4;22(1):71. doi: 10.3390/molecules22010071.
One of the major therapeutic approaches to preventing relapse and accelerating the healing of duodenal and gastric ulcers is the eradication of . Due to the emergence of antibiotic resistance among clinical strains of , alternative approaches using newly discovered antimicrobial agents in combination with the standard regimens for the treatment of 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 . 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 , with the best in vitro effect for compound . 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 showed significant urease inhibition activity with IC of 62.5 µg/mL. These results suggest that 8-nitroflouroquinolone derivatives may have a useful role in combination with anti- drugs in the management of -associated diseases.
预防十二指肠溃疡和胃溃疡复发并加速其愈合的主要治疗方法之一是根除幽门螺杆菌。由于幽门螺杆菌临床菌株中出现了抗生素耐药性，越来越需要使用新发现的抗菌药物与治疗幽门螺杆菌的标准方案相结合的替代方法。本研究的目的是研究新合成的8-硝基氟喹诺酮衍生物单独使用或与甲硝唑联合使用时对甲硝唑耐药幽门螺杆菌的作用。基于标准的抗菌药敏试验方法和棋盘滴定法，所有测试化合物对12株幽门螺杆菌临床菌株均表现出有趣的抗菌活性，其中化合物表现出最佳的体外效果。此外，一些测试化合物与甲硝唑联合使用时观察到协同和相加活性。此外，在测试的硝基氟喹诺酮衍生物中，化合物表现出显著的脲酶抑制活性，IC50为62.5 µg/mL。这些结果表明，8-硝基氟喹诺酮衍生物在与抗幽门螺杆菌药物联合用于管理幽门螺杆菌相关疾病中可能具有有益作用。
