University of Massachusetts Medical School
With over 30 different Human Immunodeficiency Virus drugs approved by the FDA, drug resistance is still a major problem. This experiment suggested a new general structure-based design for drug discovery based on the substrate envelope hypothesis in order to successfully design and synthesize a series of novel HIV-1 protease inhibitors. The design inhibitors utilize the 2-ethylbutyl group as new high affinity P1129140 ligands. The designed compounds showed highly potent inhibitory activity against wild-type and a panel of MDR HIV-1 Protease variants. Further development of these protease inhibitors may lead to more effective treatments against drug-resistant HIV-1.
Worcester Polytechnic Institute
Major Qualifying Project
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Chemistry and Biochemistry