Drug discovery for Human Immunodeficiency Virus (HIV) has resulted in life-saving therapies, making a large impact on modern medicine. However, current treatments are being met with high resistance rates towards HIV due to constant viral mutations, poor bioavailability, and patient noncompliance due to side effects. Consequently, there is an imperative need for the development of new lead compounds with lower toxicity, increased bioavailability, and higher binding affinity. Recent studies have shown boron-modified inhibitors have a higher inhibitory affinity for HIV-1 protease than the corresponding non-boron analogs. The main goal is to synthesize a library of cyclic and straight-chain boronates that may function as dual-mode, both associative and competitive, inhibitors of the HIV-1 protease. Cyclic boronates are expected to be more successful inhibitors due to their structural rigidity. The target boronates have the potential for greater affinity towards the protease enzyme, increased bioavailability, and fewer adverse side effects. In addition, the cyclic and straight-chain boronates being synthesized will serve to expand molecular diversity, as well as organoboron chemistry in general.

Exploratory synthesis of novel cyclic and straight-chain 1,3-azaborines as potential HIV-1 protease inhibitors

2019 Spring National Meeting

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