Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, and pharmaceutical compositions and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.本文提供巨環絲胺酸蛋白酶抑制劑化合物,例如式I化合物,及其醫藥組合物及製備方法。亦提供使用其治療有需要之宿主中HCV感染的方法。