Work

Pyrazole-Based Inhibitors of the Bacterial Enzyme DapE as Potential Antibiotics

Year: 2025

Type: conference-paper

Abstract: As bacteria become increasingly resistant to antibiotics, there is a need for new antibiotics using alternative pathways. To answer this need, our research investigates inhibitors of the bacterial enzyme N-succinyl-L,L-2,6-diaminopimelic acid desuccinylase (DapE). Based on previous work, we focused on pyrazole-based inhibitors, which were tested using a ninhydrin-based assay. The most potent pyrazole analog, 7d, has an IC50 of 17.9 ± 8.0 µM, and analog (R)-7q is a competitive inhibitor with an IC50 of 18.8 µM. A thermal shift assay demonstrated stabilization of the enzyme after binding with inhibitor (R)-7q and a Ki of 17.3 ± 2.8 µM.

Source: Loyola eCommons (Loyola University of Chicago)

Authors: Bland, Alayna, Kelley, Emma H, DiPuma, Thomas, Thabthimthong, Teerana, Becker, Daniel P.

Language: English

Topic: Synthesis and Biological Evaluation

Subfield: Organic Chemistry

Field: Chemistry

Domain: Physical Sciences

Open Access status: green

OpenAlex ID: W7051906053

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