Dihydroquinazoline-Derived Inhibitors for Alzheimer's Disease Treatment

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Alzheimer's disease is a progressive mental deterioration, resulting in loss of memory, confusion and disorientation, and other behavioral problems. Unfortunately, no definitive cure has been developed to treat this disease. Beta-secretase, an important enzyme in the development and onset of Alzheimer's disease, contributes to the formation of amyloid-beta peptides that aggregate in the brain of Alzheimer's patients. Blocking beta-secretase is a potential strategy for the treatment of Alzheimer's disease.

Researchers at Purdue University have developed novel compounds that inhibit beta-secretase for Alzheimer's treatment. By focusing on a known dihydroquinazoline scaffold, a series of novel dihydroquinazoline derivatives were synthesized and evaluated. Several compounds in this series were shown to exhibit better beta-secretase cellular inhibitory activity compared to current compounds reported in literature. These compounds show increased potency, improved aqueous solubility, increased metabolic stability, and improved oral bioavailability.

Advantages:
-Improved beta-secretase cellular inhibition
-Increased metabolic stability

Potential Applications:
-Medical/Health
-Pharmaceutical industry
Sep 22, 2011
Utility Patent
United States
8,394,807
Mar 12, 2013

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Purdue Office of Technology Commercialization
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