More Potent and Metabolically Stable HIV/AIDS Therapeutics
- 总结
- Researchers at Purdue University have developed a series of alkenyldiarylmethane (ADAM) NNRTIs that inhibit the cytopathic effect of HIV-1 in CEM-SS cells and MT-4 cells and offer potential value in the treatment of AIDS. These ADAMs were developed through research on an original 25 ADAMs tested with different methyl ester bioisosteres at three different locations. This research resulted in inhibitors proven to be more potent and designed to be more metabolically stable than the original lead compound. This new series of compounds also includes an inhibitor effective against the resistant K103N mutant reverse transcriptase.
- 技术优势
- More potent inhibitor Metabolically stable K103N mutant inhibitor
- 技术应用
- AIDS/HIV treatment Research & Development
- 详细技术说明
- Mark CushmanPurdue Medicinal Chemistry and Molecular Pharmacology
- *Abstract
-
- *Background
- Current modes of AIDS treatment involve anti-HIV agents that are entry inhibitors, fusion inhibitors, integrase inhibitors, protease inhibitors, or reverse transcriptase inhibitors. Reverse transcriptase inhibitors fall into two categories, nucleoside reverse transcriptase inhibitors (NRTIs) and non-nucleoside reverse transcriptase inhibitors (NNRTIs). Unfortunately, mutations in the HIV reverse transcriptase lead to NNRTIs becoming ineffective and current NNRTIs can be easily inactivated by human metabolism. To overcome these challenges, new inhibitors are necessary.
- *IP Issue Date
- None
- *IP Type
- Provisional
- *Stage of Development
- Proof of concept
- *Web Links
- Purdue Office of Technology CommercializationPurdueInnovation and EntrepreneurshipMark CushmanPurdue Medicinal Chemistry and Molecular Pharmacology
- 国家
- United States
- 申请号码
- None
- 国家/地区
- 美国
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