{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,8,29]],"date-time":"2026-08-29T16:10:47Z","timestamp":1788019847046,"version":"build-2784847793"},"reference-count":40,"publisher":"MDPI AG","issue":"2","license":[{"start":{"date-parts":[[2024,1,22]],"date-time":"2024-01-22T00:00:00Z","timestamp":1705881600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"Loyola University Office of Research Services (ORS) Internal Research Award (IRA)","award":["IPRS# 1083"],"award-info":[{"award-number":["IPRS# 1083"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["IJMS"],"abstract":"<jats:p>Based on our previous success in using cyclobutanone derivatives as enzyme inhibitors, we have designed and prepared a 37-member library of \u03b1-aminocyclobutanone amides and sulfonamides, screened for inhibition of the bacterial enzyme diaminopimelate desuccinylase (DapE), which is a promising antibiotic target, and identified several inhibitors with micromolar inhibitory potency. Molecular docking suggests binding of the deprotonated hydrate of the strained cyclobutanone, and thermal shift analysis with the most potent inhibitor (3y, IC50 = 23.1 \u00b5M) enabled determination of a Ki value of 10.2 +\/\u2212 0.26 \u00b5M and observed two separate Tm values for H. influenzae DapE (HiDapE).<\/jats:p>","DOI":"10.3390\/ijms25021339","type":"journal-article","created":{"date-parts":[[2024,1,22]],"date-time":"2024-01-22T05:42:31Z","timestamp":1705902151000},"page":"1339","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":8,"title":["Cyclobutanone Inhibitors of Diaminopimelate Desuccinylase (DapE) as Potential New Antibiotics"],"prefix":"10.3390","volume":"25","author":[{"given":"Thahani S.","family":"Habeeb Mohammad","sequence":"first","affiliation":[{"name":"Department of Chemistry and Biochemistry, Loyola University Chicago, 1032 West Sheridan Road, Chicago, IL 60660, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-3638-7628","authenticated-orcid":false,"given":"Emma H.","family":"Kelley","sequence":"additional","affiliation":[{"name":"Department of Chemistry and Biochemistry, Loyola University Chicago, 1032 West Sheridan Road, Chicago, IL 60660, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-5076-0150","authenticated-orcid":false,"given":"Cory T.","family":"Reidl","sequence":"additional","affiliation":[{"name":"Department of Chemistry and Biochemistry, Loyola University Chicago, 1032 West Sheridan Road, Chicago, IL 60660, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Katherine","family":"Konczak","sequence":"additional","affiliation":[{"name":"Department of Chemistry and Biochemistry, Loyola University Chicago, 1032 West Sheridan Road, Chicago, IL 60660, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Megan","family":"Beulke","sequence":"additional","affiliation":[{"name":"Department of Chemistry and Biochemistry, Loyola University Chicago, 1032 West Sheridan Road, Chicago, IL 60660, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Janielle","family":"Javier","sequence":"additional","affiliation":[{"name":"Department of Chemistry and Biochemistry, Loyola University Chicago, 1032 West Sheridan Road, Chicago, IL 60660, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kenneth W.","family":"Olsen","sequence":"additional","affiliation":[{"name":"Department of Chemistry and Biochemistry, Loyola University Chicago, 1032 West Sheridan Road, Chicago, IL 60660, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-9392-0460","authenticated-orcid":false,"given":"Daniel P.","family":"Becker","sequence":"additional","affiliation":[{"name":"Department of Chemistry and Biochemistry, Loyola University Chicago, 1032 West Sheridan Road, Chicago, IL 60660, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2024,1,22]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"1763","DOI":"10.1001\/jama.298.15.1763","article-title":"Invasive Methicillin-Resistant Staphylococcus Aureus Infections in the United States","volume":"298","author":"Klevens","year":"2007","journal-title":"JAMA J. 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