Maltase-glucoamylase (MGA) is an enzyme of glycoside hydrolase Family 31. It is an alpha-glucosidase anchored in the membrane of small intestinal epithelial cells responsible for the final step of mammalian starch digestion causing the release of glucose. Inhibitors targeting MGA and other alpha-glucosidases delay glucose production following digestion and are currently used in treatment of Type II diabetes. In an effort to discover new inhibitors that may aid in diabetes treatment and prevention, analogs of known inhibitors are being designed and synthesized. This thesis reports the use of Drosophila tissue culture for production and purification of active human recombinant MGA suitable for structural, kinetic and inhibition studies. Four promising inhibitors were discovered from a group of prospective inhibitors modeled after salacinol, a naturally occurring alpha-glucosidase inhibitor, and miglitol, a currently prescribed anti-diabetic. Future work will focus on the structural analysis of MGA as well as drug design for new anti-diabetics.