Title

Towards the synthesis of novel boronates as potential HIV-1 protease inhibitors

Document Type

Oral Presentation

Location

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.

Poster Number

23

Faculty Mentor(s)

Levente Fabry-Asztalos

Additional Mentoring Department

Chemistry

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May 17th, 8:30 AM May 17th, 11:00 AM

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.