Current therapies for toxoplasmosis rely on a few drugs, most of which have severe side effects, and seeking ideal therapies for different types of toxoplasmosis is a longterm and challenging mission. Research and development (R&D) of novel drugs against Toxoplasma gondii (T. gondii) has focused on two main directions, the structural modification of lead compounds and natural products. Here we summarize the recent advances in the development of anti-T. gondii drugs from these two perspectives and provide comprehensive insights, reflecting on the advantages and selected molecules in each field. This review also focuses on the current obstacles to the development of novel anti-T. gondii agents, proposes comprehensive solutions, and facilitates future development.
■ SIGNIFICANCE• The detailed analysis of current advances on anti-T.gondii drugs was discussed from structural modification of lead compounds and natural products. • Rules associated with anti-T. gondii drug activities and important novel anti-T. gondii objectives are highlighted, which is essential for effective prevention and treatment of toxoplasmosis. • This perspective focuses on the obstacles in the development of novel anti-T. gondii agents based on research progress and provides comprehensive solutions.