Background: The use of antibiotics has compromised due to the appearance of multidrug- resistant strains and decreased susceptibility of strains to antibiotics. Antibiotic resistance has become a worldwide threat as well as Helicobacter pylori induced gastric cancer is a major problem nowadays. Therefore, it is the need of time to synthesize potent anti-urease motifs.

Introduction: Schiff bases represent a large class of biologically active compounds that exhibited a broad spectrum of biological activities. Amikacin is an important drug used against multidrugresistant species of microbes. Therefore, imine derivatives of amikacin may help to reduce the resistance of microbes and to treat the Helicobacter pylori induced stomach problems by inhibiting the Helicobacter Pylori Urease enzyme.

Methods: Schiff bases of amikacin were synthesized and screened for in-vitro antibacterial assay performed by well diffusion method against Bacillus megaterium (Bm), Bacillus subtilis (Bs), Stenotrophomonas maltophilia (Sm), Staphylococcus aureus (Sa), Micrococcus luteus (Ml), Serratia marcescens (S. mar), Escherichia coli (E. coli) and anti-urease activity was performed by Indophenol method. Structures confirmed by IR, 1HNMR and 13CNMR spectroscopy.

Results: Compounds showed varying degrees of antibacterial effects. Schiff bases A2 and A8 exhibited potent urease inhibition activity with Ki values 0.2754 and 0.2908 μM, respectively and their binding affinity was calculated as greater than the standard drug.

Conclusion: Derivatives of amikacin with aromatic rings were more active antibacterials than those with an aliphatic side chain. The potent anti-urease activity has been recorded for compounds A2 and A8. Therefore, they may serve as lead compounds in the discovery of Helicobacter pylori Urease inhibitors.

背景：由于出现了多药耐药菌株，并且菌株对抗生素的敏感性降低，因此抗生素的使用受到了影响。抗生素耐药性已成为全球性的威胁，而幽门螺杆菌诱发的胃癌已成为当今的主要问题。因此，需要时间来合成有效的抗脲酶基序。

简介：希夫碱代表一大类具有广泛生物活性的生物活性化合物。阿米卡星是一种重要的药物，可抗多种药物的微生物。因此，阿米卡星的亚胺衍生物可以通过抑制幽门螺杆菌脲酶来帮助降低微生物的抵抗力，并治疗幽门螺杆菌引起的胃部疾病。

方法：合成阿米卡星希夫碱，并通过孔扩散法对大芽孢杆菌，枯草芽孢杆菌，嗜麦芽窄食单胞菌，金黄色葡萄球菌，金黄色微球菌进行体外抗菌测定。 ），粘质沙雷氏菌（S.mar），大肠杆菌（E.coli）和抗脲酶活性通过吲哚酚法进行。通过IR，1HNMR和13CNMR光谱确认的结构。

结果：化合物显示出不同程度的抗菌作用。Schiff碱A2和A8分别显示出有效的脲酶抑制活性，Ki值分别为0.2754和0.2908μM，计算出它们的结合亲和力大于标准药物。

结论：具有芳香环的阿米卡星衍生物比具有脂肪族侧链的衍生物具有更高的活性。已经记录了化合物A2和A8的有效抗脲酶活性。因此，它们可作为发现幽门螺杆菌脲酶抑制剂的先导化合物。