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