Obesity is an issue of great concern to people all over the world. It is accompanied by serious complications, leading to reduced quality of life and higher morbidity and mortality. Over the past few years, there has been an explosion in knowledge about the roles of potential therapeutic agents in obesity management. Among them, amino acid (AA) derivatives, such as taurine, glutathione (GSH), betaine, α-ketoglutarate (AKG), β-aminoisobutyric acid (BAIBA), and β-hydroxy-β-methylbutyrate (HMB), have recently gained popularity due to their beneficial effects on the promotion of weight loss and improvement in the lipid profile. The mechanisms of action of these derivatives mainly include inhibiting adipogenesis, increasing lipolysis, promoting brown/beige adipose tissue (BAT) development, and improving glucose metabolism. Therefore, this review summarizes these AA derivatives and the possible mechanisms responsible for their anti-obesity effects. Based on the current findings, these AA derivatives could be potential therapeutic agents for obesity and its related metabolic diseases.