Design of New Potent Class of HIV-1 Protease Inhibitors for Treatment of HIV/AIDS

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Researchers at Purdue have developed a novel series of compounds using structure-based design that show significant inhibition of HIV-1 protease. Current anti-retroviral drugs are contending with new drug-resistant strains of HIV-AIDS and have several major side effects associated with the cardiovascular and central nervous system. In order to provide new treatment options, researchers have developed a series of novel compounds by maximizing hydrogen bonding interactions with the active site protease backbone atoms.

The series of compounds made by researchers at Purdue incorporated derivatives of nilotinib-like pyridyl pyrimidinyl groups and thiazole heterocycles in combination with the hydroxyethylamine sulfonamide isostere group of the HIV-1 protease inhibitor darunavir. The researchers tested the enzyme inhibitory ability and the IC50 of each molecule and found that several had inhibitory activity at the nanomolar and sub-nanomolar level as well as antiviral activity at the low nanomolar level.

Technology Validation:
- Enzyme inhibitory activity of molecules verified through an enzyme-inhibitory assay with HIV protease.
- Antiviral activity of molecules validated with MT-2 human-T-lymphoid cells model with HIVLAI.

- Select compounds among series have better and/or comparable antiviral and enzyme inhibitory activity of HIV and HIV-1 protease.
- Distinct chemical structure from other commercial HIV protease inhibitors, potentially more difficult for new strains to develop resistance to new series of compounds.

- HIV/AIDS treatment: New series of compounds could be developed into anti-retroviral drugs against multi-drug resistant strains of HIV.
- HIV/AIDS diagnostics: Fluorophores could be bound to compounds and be used to visualize distribution of HIV-1 protease within cells.
Mar 24, 2023
Provisional-Gov. Funding
United States
Purdue Office of Technology Commercialization
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