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Novel Bicyclic CCR5 Antagonists for Treatment of HIV/AIDS

总结: Purdue University researchers developed Darunavir, brand name Prezista, a drug used to treat HIV infection. Prezista was developed by the pharmaceutical company Tibotec and is an OARAC recommended treatment option for treatment-naïve and treatment-experienced adults and adolescents. It is also used in patients with drug-resistant HIV. They have also developed a new generation of protease inhibitors that are exceedingly potent and maintain potency against multidrug resistant HIV-1 variants. Dr. Ghosh's laboratory has designed, synthesized, and evaluated several different series of compounds. These novel protease inhibitors show potent enzyme inhibitory, antiviral activity, and exceptional broad-spectrum activity against highly cross-resistant mutant.

技术优势: Decreased adverse side effectsEffective against multidrug resistant HIV-1 variants Improved bioavailabilitySuperior pharmacokinetic properties

*Background: Advances in the treatment of HIV-AIDS with HIV-1 protease inhibitors in combination with reverse transcriptase inhibitors, known as highly active antiretroviral therapy (HAART), has resulted in improved life expectancy and significantly reduced HIV/AIDS-related mortality in the developed world. Unfortunately, HAART suffers from adverse drug side effects, poor oral bioavailability, and drug interactions. In addition, drug-resistant HIV-1 variants have begun to emerge. Development of antiretroviral therapy with broad-spectrum activity and minimal side effects is needed for current and future HIV/AIDS treatment

*Web Links: Purdue Office of Technology CommercializationPurdueInnovation and EntrepreneurshipArun GhoshGhosh GroupPurdue Chemistry

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