The chronic metabolic disorder known as diabetes mellitus is linked to a wide range of complications, the most prominent of which is diabetic neuropathy, which has a significant impact on the quality-of life people who have diabetes experience. The current treatment strategies frequently fail to be effective and require the utilization of distinct therapies for the control of glycemic levels and the protection of nerves. This results in difficulties in patient compliance and maintenance of the condition. The potential of dual-action drugs, which are drugs that combine neuroprotective and anti-diabetic properties into a single formulation, is investigated. The mechanistic synergy that exists between the regulation of glucose and the health of nerves, we bring to light the rationale behind a combined therapeutic approach. As a means of developing effective compounds that are tailored to diabetic environments, a number of novel synthetic strategies are being discussed. These strategies include multifunctional drug design, pharmacophore hybridization, and the prodrug approach. Additional support for the development of this field comes from the identification of important chemical scaffolds, as well as from the utilization of contemporary synthetic techniques.