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Medicine and Health Sciences Commons

Open Access. Powered by Scholars. Published by Universities.®

2012

Electronic Theses and Dissertations

AIDS

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Design And Synthesis Of Hiv-1 Integrase Inhibitors, Sarah Chajkowski Scarry Jan 2012

Design And Synthesis Of Hiv-1 Integrase Inhibitors, Sarah Chajkowski Scarry

Electronic Theses and Dissertations

In recent years, HIV-1 integrase (IN) has emerged as an attractive target for the treatment of human immunodeficiency virus type 1 (HIV-1), the causative pathogen of acquired immuno-deficiency syndrome (AIDS). Several classes of IN inhibitors are known but many of these compounds are toxic, do not show antiviral activity or display decreased potency. Therefore, new classes of potent IN inhibitors are desperately needed. The b-diketo (b-DK) class of compounds has emerged as one of the most successful classes of IN inhibitors. Although several b-DK inhibitors with potent antiviral activity are known, compounds containing b-DK motifs have limitations in drug development. …