Abstract: As an interdisciplinary frontier discipline at the intersection of chemistry, pharmacy, and life sciences, the specialized course of medicinal chemistry plays a pivotal role in cultivating versatile talents. However, current teaching practices face challenges such as outdated curriculum content, monotonous teaching methods, and insufficient integration of ideological and political education. By fully incorporating course-based ideological and political education with a strong emphasis on “patriotism and professional responsibility”, deepening the interdisciplinary integration of organic chemistry and drug design to “strengthen fundamentals and enhance qualities”, and leveraging virtual simulations, AI technologies, and industry-university collaborations to establish a multi-tiered practical training system to “foster practice-driven education and innovative capabilities,” students’ innovative thinking, practical skills, and social responsibility have been significantly enhanced.