The relationship between entrepreneurship and sustainable development has received considerable attention from academics and policymakers, as society searches for solutions leading to sustainability. The role of innovation and institutional quality in reaching sustainability goals is one of the key areas tackled by the current sustainable development debate, particularly in developing countries. Using a modified environmental Kuznets curve model, this study attempts to better improve our understanding of the critical roles of innovation, institutional quality, and entrepreneurship in the structural change toward a sustainable future in Africa. The empirical results show that both formal and informal entrepreneurship are conducive to less environmental quality and sustainability in 17 African countries where the contribution of informal entrepreneurship is much higher compared to the formal one. However, the relationship between entrepreneurship and sustainable development becomes strongly positive when the levels of innovation and institutional quality are higher. This research makes a contribution to this important emerging research area in that it clarifies conditions through which countries and firms in Africa can move toward more sustainable products and services. Formalizing the informal sector can lead to the improvement of the environmental and economic performance.