Executive Summary : | Aminoglycoside based antibiotic's bacteriological and clinical efficacy has decreased recently due to antimicrobial resistance in patient body. The development of antimicrobial resistance meant that their effectiveness had a limited term so that improper and indefensible use of them helped to generate and propagate antibiotic-resistant pathogens which makes antibiotic resistance as global problem. To exhibit antibacterial activity of aminoglycoside antibiotics must bind to the RNA receptor located within the cell which requires uptake of the aminoglycoside antibiotics by the bacterial cell. To enhance the uptake of aminoglycoside into the bacterial cell, PIam interested in the synthesis of aminoglycoside-nucleolipid conjugates.The nucleolipids in thought are cationic in nature which will be developed to facilitate transport through membranes. Co-administration of aminoglycoside with cationic nucleolipid may induce synergistic effects resulting in enhanced antimicrobial activity which feature will make aminoglycoside-nucleolipid conjugates as attractive targets for antimicrobial drug discovery, development of novel antiseptics, and prevention of biofilms. The readily available aminoglycoside sulphate will be converted to such a functional group so that conjugation with cationic nucleolipid will be feasible and high yielding. Synthesized aminoglycoside-nucleolipid conjugates will be purified by column chromatography and will be characterized by NMR, HRMS/MALDI and other spectroscopic techniques. After synthesis of desired aminoglycoside-nucleolipid conjugates the bacterial assays against Gram-positive strains e.g S. aureus, MRSA, Staphylococcus epidermidis, methicillin-resistant S. epidermidis (MRSE), Streptococcus pneumoniae and Gram-negative strains e.g. Escherichia coli, gentamicin resistant E. coli, and Pseudomonas aeruginosa will be studied to determine minimum inhibitory concentrations (MIC) in μg/mL. |