Novel Dihydroquinazoline-Derived Memapsin 2 Inhibitors for Treatment of Alzheimer's Disease

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

TRL: 2

Intellectual Property:

Keywords: Alzheimer's disease treatment, Beta-secretase inhibitor, amyloid-beta peptides, progressive mental deterioration, dihydroquinazoline scaffold, dihydroquinazoline derivatives, cellular inhibitory activity, improved aqueous solubility, increased metabolic stability, oral bioavailability, Alzheimer's Disease, Drug Development, Medical/Health, Pharmaceuticals