Document Type

Thesis

Date of Degree Completion

Spring 2008

Degree Name

Bachelor of Science

Department

Chemistry

Committee Chair

Dr. Levente Fabry-Astalos, Department of Chemistry

Second Committee Member

Dr. JoAnn Peters

Third Committee Member

Dr. Andrew A. Piacsek, Science Honors Research Program

Abstract

Drug discovery has resulted in many life-saving therapies, making a great impact on modem medicine and the human condition. Even though new therapies are available many drugs are highly susceptible to resistance development, have poor bioavailability, and some of them are toxic. HIV-I protease inhibitors presently on the market show high specificity but have low bioavailability and high toxicity. Furthermore, the available drugs have a very low affinity for mutant forms of HIV -1 protease. Recent studies have shown that boronated HIV-I protease inhibitors, which demonstrate both competitive and associative inhibition, have a higher affinity for HIV-I protease at lower concentrations than their corresponding carbon analogs and also inhibit a mutant form of HIV-I protease. In this study nine novel I,3-azaborine type of heterocycles are being synthesized. Their biological characteristics will be analyzed and compared with other inhibitors to determine their effectiveness as potential novel anti-HIV drugs.

Comments

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