Towards the Synthesis of Novel Boronates as Potential HIV-1 Protease Inhibitors

Human Immunodeficiency Virus (HIV) is a transmissible pathogen that negatively impacts nearly 38 million lives globally. The virus attacks the host’s white blood (CD4) cells to successfully replicate viral genetic information. Retroviral aspartyl protease HIV-1 hydrolyses peptide bonds of host’s dsDNA in which HIV’s genetic material is then integrated, resulting in new viral particles. The infected immune T cells replicate abnormally when they undergo cell division stages. Consequently, the immune system of the infected host weakens, resulting in increased vulnerability to other infections and diseases. HIV pathogens can develop antiviral drug resistance via genetic mutations; therefore, development of new HIV medicine is essential for effective antiretroviral therapy (ART). Antiretroviral therapy (ARTs) suppresses HIV and rapidly replicates peripheral blood CD4 T-cell count, reversing immunodeficiency. HIV-1 protease inhibitors are believed to reduce the development of HIV into Acquired Immunodeficiency Syndrome (AIDS) by blocking and preventing protease from hydrolyzing viral proteins that are needed for successful viral replication. In this work we are proposing the synthesis of cyclic 1,3-azaborines. These compounds are designed to potentially act in dual mode, as competitive and as associative inhibitors of HIV-1 protease