Over the last few decades, many researchers have investigated in detail the characteristics of bioactive compounds such as polyphenols, vitamins, flavonoids, and glycosides, and volatile compounds in fruits, vegetables and medicinal and aromatic plants that possess beneficial properties, as well as consumer acceptance and preference. The main aim of this article is to provide an updated overview of recent research endeavors related to the effects of the drying process on the major bioactive/effective compounds in agricultural products. Particular emphasis was placed on details related to the changes occurring in vitamin C, polyphenols, flavonoids, glycosides and volatile compounds, as well as the antioxidant activity. An analysis of the degradation mechanisms of these compounds showed that vitamin C, phenols, flavonoids and glycosides react with oxygen during the convective drying process under high drying temperatures, and the reaction rate results in degradation in such bioactive compounds due to high reducibility. On the other hand, high temperature results in a short drying time, thus minimizing the degradation of bioactive compounds. The reviewed research works addressing this trend revealed that the ideal drying temperatures for retaining vitamin C, polyphenols, flavonoids, glycosides, volatile compounds and their antioxidant activity were 50–60 °C, 55–60 °C, 60–70 °C, 45–50 °C, 40–50 °C and 50–70 °C, respectively. In conclusion, to maintain plant bioactive components, convective drying at relatively low drying temperatures is strongly recommended.