Towards the synthesis of novel boronates as potential HIV-1 protease inhibitors
Document Type
Oral Presentation
Campus where you would like to present
SURC Ballroom A
Start Date
17-5-2012
End Date
17-5-2012
Abstract
Drug discovery for HIV/AIDS has resulted in many life-saving therapies, making a profound impact on modern medicine. Current drug therapies exist, but are susceptible to resistance development, have poor bioavailability, and cause several side effects. For this reason, there is an urgent need to develop new types of inhibitors that address those problems. We are synthesizing novel boronates as potential dual-mode, competitive and associative, inhibitors of HIV-1 protease. Recent studies showed that boron-modified inhibitors have a higher affinity for the protease than their corresponding non-boronated analogs. Furthermore, the boron-modified structures were inhibitory to an HIV-1 protease variant that is resistant to several HIV-1 protease inhibitors. A library of both straight chain and cyclic boronates are being synthesized.
Recommended Citation
Frank, Michael; Faulkner, Andrea; Jennings, Julia; Sigurjonsson, Kristin; and Schreiber, John, "Towards the synthesis of novel boronates as potential HIV-1 protease inhibitors" (2012). Symposium Of University Research and Creative Expression (SOURCE). 42.
https://digitalcommons.cwu.edu/source/2012/posters/42
Poster Number
23
Additional Mentoring Department
Chemistry
Towards the synthesis of novel boronates as potential HIV-1 protease inhibitors
SURC Ballroom A
Drug discovery for HIV/AIDS has resulted in many life-saving therapies, making a profound impact on modern medicine. Current drug therapies exist, but are susceptible to resistance development, have poor bioavailability, and cause several side effects. For this reason, there is an urgent need to develop new types of inhibitors that address those problems. We are synthesizing novel boronates as potential dual-mode, competitive and associative, inhibitors of HIV-1 protease. Recent studies showed that boron-modified inhibitors have a higher affinity for the protease than their corresponding non-boronated analogs. Furthermore, the boron-modified structures were inhibitory to an HIV-1 protease variant that is resistant to several HIV-1 protease inhibitors. A library of both straight chain and cyclic boronates are being synthesized.
Faculty Mentor(s)
Levente Fabry-Asztalos