Presenter Information

Katie Jane TormaFollow

Major

Chemistry

Anticipated Graduation Year

2021

Access Type

Open Access

Abstract

Due to the increase in antibacterial resistance, there is an urgent need for new and novel antibacterial drugs. The target enzyme for this project is the dapE-encoded bacterial enzyme N-succinyl-L,L-diaminopimelic acid desuccinylase (DapE). DapE is a key enzyme in the synthesis of bacterial cellular walls via the lysine biosynthetic pathway. DapE inhibitors should selectively target bacterial DapE which will be lethal to bacteria with no mechanism-based toxicity in humans due to the absence of the lysine biosynthetic pathway in mammals. Thus DapE enzyme is an ideal target for novel antibiotics. The lead molecules identified by the Becker lab via a High-Throughput screen include the tetrazole, (2-[(1-phenyl-1H-tetrazol-5-yl)sulfanyl]-N-(1,3-thiazol-2-yl)propanamide). Synthesis of new analogs of this lead molecule will be described.

Faculty Mentors & Instructors

Thahani S. Habeeb Mohammad and Dr. Daniel P. Becker

Creative Commons License

Creative Commons License
This work is licensed under a Creative Commons Attribution-Noncommercial-No Derivative Works 3.0 License.

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Synthesis of Tetrazole-Based DapE Inhibitors as Potential Antibiotics

Due to the increase in antibacterial resistance, there is an urgent need for new and novel antibacterial drugs. The target enzyme for this project is the dapE-encoded bacterial enzyme N-succinyl-L,L-diaminopimelic acid desuccinylase (DapE). DapE is a key enzyme in the synthesis of bacterial cellular walls via the lysine biosynthetic pathway. DapE inhibitors should selectively target bacterial DapE which will be lethal to bacteria with no mechanism-based toxicity in humans due to the absence of the lysine biosynthetic pathway in mammals. Thus DapE enzyme is an ideal target for novel antibiotics. The lead molecules identified by the Becker lab via a High-Throughput screen include the tetrazole, (2-[(1-phenyl-1H-tetrazol-5-yl)sulfanyl]-N-(1,3-thiazol-2-yl)propanamide). Synthesis of new analogs of this lead molecule will be described.