The clinically used potent broad spectrum bactericidal aminoglycosides (AGs) antibiotics have suffered a diminished use due to the dose-related toxicity and rapid emergence of resistance. To overcome these shortfalls, researchers have performed many structural modifications on the aminoglycoside scaffold. The motivation behind the development of novel aminoglycoside analogs is in part caused by the inability to discover novel antibiotics with new modes of action especially against Gram-negative bacteria. As AGs comprise of highly functionalised polycationic oligosaccharides carrying several hydroxy and amino functional groups with an incorporated streptamine unit, numerous synthetic approaches for their fabrication and revitalization have been articulated. Impressive endeavours and advancements made in this direction by researchers across the globe have been well documented in a large volume of literature. The objective of this review article is to summarize in a comprehensive manner recent progress in this field with a special attention to the chemistry of structurally related neomycin, paromomycin and neamine.