{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,26]],"date-time":"2026-09-26T03:43:01Z","timestamp":1790394181098,"version":"4.1.0"},"reference-count":36,"publisher":"Wiley","issue":"7","license":[{"start":{"date-parts":[[2025,1,14]],"date-time":"2025-01-14T00:00:00Z","timestamp":1736812800000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"funder":[{"DOI":"10.13039\/501100012226","name":"Fundamental Research Funds for the Central Universities","doi-asserted-by":"publisher","id":[{"id":"10.13039\/501100012226","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100003395","name":"Shanghai Municipal Education Commission","doi-asserted-by":"publisher","award":["2021 Sci"],"award-info":[{"award-number":["2021 Sci"]}],"id":[{"id":"10.13039\/501100003395","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100003395","name":"Shanghai Municipal Education Commission","doi-asserted-by":"publisher","award":["Tech 03-28"],"award-info":[{"award-number":["Tech 03-28"]}],"id":[{"id":"10.13039\/501100003395","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["chemistry-europe.onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["ChemMedChem"],"published-print":{"date-parts":[[2025,4]]},"abstract":"<jats:title>Abstract<\/jats:title>\n                  <jats:p>\n                    The expression of\n                    <jats:italic>Klebsiella pneumoniae<\/jats:italic>\n                    carbapenemase (KPC), a type of carbapenem\u2010hydrolyzing \u03b2\u2010lactamase, in Gram\u2010negative bacteria has caused significant bacterial resistance to carbapenems, the antibiotic of last resort. Herein, we describe the discovery of 2\u2010carboxyquinoline boronic acids as inhibitor of KPC. We have identified fluoro\u2010substituted carboxyquinoline boronic acids\n                    <jats:bold>1\u2009e<\/jats:bold>\n                    as the most potent inhibitor, with an IC\n                    <jats:sub>50<\/jats:sub>\n                    of 8.3\u2005nM for KPC\u20102, while this compound is significantly less efficient at reducing the activity of other \u03b2\u2010lactamases. This compound proved to have low cytotoxicity towards mammalian cells, as well as low haemolysis and antibacterial activity. However,\n                    <jats:bold>1\u2009e<\/jats:bold>\n                    potentiated the efficacy of \u03b2\u2010lactam antibiotics (e.\u2009g., meropenem and ceftazidime) against KPC\u20102\u2010expressing resistant\n                    <jats:italic>Klebsiella pneumonia<\/jats:italic>\n                    by up to 256\u2010fold.\n                  <\/jats:p>","DOI":"10.1002\/cmdc.202400901","type":"journal-article","created":{"date-parts":[[2024,12,27]],"date-time":"2024-12-27T04:53:50Z","timestamp":1735275230000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":2,"title":["2\u2010Carboxyquinoline Boronic Acids as Highly Potent KPC Inhibitors"],"prefix":"10.1002","volume":"20","author":[{"given":"Zheng","family":"Ma","sequence":"first","affiliation":[{"name":"State Key Laboratory of Bioreactor Engineering, Shanghai Key Laboratory of New Drug Design, Frontiers Science Center for Materiobiology and Dynamic Chemistry, Shanghai Frontier Science Research Base of Optogenetic Techniques for Cell Metabolism, School of Pharmacy East China University of Science and Technology  Shanghai 200237 P.R. China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ge","family":"Cui","sequence":"additional","affiliation":[{"name":"State Key Laboratory of Bioreactor Engineering, Shanghai Key Laboratory of New Drug Design, Frontiers Science Center for Materiobiology and Dynamic Chemistry, Shanghai Frontier Science Research Base of Optogenetic Techniques for Cell Metabolism, School of Pharmacy East China University of Science and Technology  Shanghai 200237 P.R. China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lijie","family":"Dou","sequence":"additional","affiliation":[{"name":"State Key Laboratory of Bioreactor Engineering, Shanghai Key Laboratory of New Drug Design, Frontiers Science Center for Materiobiology and Dynamic Chemistry, Shanghai Frontier Science Research Base of Optogenetic Techniques for Cell Metabolism, School of Pharmacy East China University of Science and Technology  Shanghai 200237 P.R. China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Fangfang","family":"Chen","sequence":"additional","affiliation":[{"name":"State Key Laboratory of Bioreactor Engineering, Shanghai Key Laboratory of New Drug Design, Frontiers Science Center for Materiobiology and Dynamic Chemistry, Shanghai Frontier Science Research Base of Optogenetic Techniques for Cell Metabolism, School of Pharmacy East China University of Science and Technology  Shanghai 200237 P.R. China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-1033-9211","authenticated-orcid":false,"given":"Hexin","family":"Xie","sequence":"additional","affiliation":[{"name":"State Key Laboratory of Bioreactor Engineering, Shanghai Key Laboratory of New Drug Design, Frontiers Science Center for Materiobiology and Dynamic Chemistry, Shanghai Frontier Science Research Base of Optogenetic Techniques for Cell Metabolism, School of Pharmacy East China University of Science and Technology  Shanghai 200237 P.R. China"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2025,1,14]]},"reference":[{"key":"e_1_2_8_1_1","doi-asserted-by":"publisher","DOI":"10.1038\/510477a"},{"key":"e_1_2_8_2_1","unstructured":"W.\u2005H. Organization Prioritization of Pathogens to Guide Discovery Research and Development of New Antibiotics for Drug-Resistant Bacterial Infections Including Tuberculosis.2017."},{"key":"e_1_2_8_3_1","doi-asserted-by":"publisher","DOI":"10.1021\/cr030102i"},{"key":"e_1_2_8_4_1","doi-asserted-by":"publisher","DOI":"10.1128\/CMR.00037-09"},{"key":"e_1_2_8_5_1","doi-asserted-by":"publisher","DOI":"10.1177\/1060028014556652"},{"key":"e_1_2_8_6_1","doi-asserted-by":"publisher","DOI":"10.1101\/cshperspect.a025247"},{"key":"e_1_2_8_7_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.jmedchem.9b01279"},{"key":"e_1_2_8_8_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.accounts.0c00863"},{"key":"e_1_2_8_9_1","doi-asserted-by":"publisher","DOI":"10.1097\/MRM.0000000000000106"},{"key":"e_1_2_8_10_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.mib.2011.07.026"},{"key":"e_1_2_8_11_1","doi-asserted-by":"publisher","DOI":"10.1093\/cid\/ciad095"},{"key":"e_1_2_8_12_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.apsb.2021.01.010"},{"key":"e_1_2_8_13_1","doi-asserted-by":"publisher","DOI":"10.3390\/molecules27092615"},{"key":"e_1_2_8_14_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bmc.2022.116748"},{"key":"e_1_2_8_15_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.jmedchem.5b00127"},{"key":"e_1_2_8_16_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.jmedchem.9b01518"},{"key":"e_1_2_8_17_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.jmedchem.9b01976"},{"key":"e_1_2_8_18_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.jmedchem.1c00437"},{"key":"e_1_2_8_19_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.jmedchem.9b00735"},{"key":"e_1_2_8_20_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bmcl.2004.05.054"},{"key":"e_1_2_8_21_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2022.114571"},{"key":"e_1_2_8_22_1","doi-asserted-by":"publisher","DOI":"10.3390\/molecules28217362"},{"key":"e_1_2_8_23_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2022.114174"},{"key":"e_1_2_8_24_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.jmedchem.3c00171"},{"key":"e_1_2_8_25_1","doi-asserted-by":"publisher","DOI":"10.1038\/nchem.1435"},{"key":"e_1_2_8_26_1","doi-asserted-by":"publisher","DOI":"10.1021\/jm400769b"},{"key":"e_1_2_8_27_1","doi-asserted-by":"publisher","DOI":"10.1039\/B610213C"},{"key":"e_1_2_8_28_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.jmedchem.5b00258"},{"key":"e_1_2_8_29_1","doi-asserted-by":"publisher","DOI":"10.1128\/aac.02414-21"},{"key":"e_1_2_8_30_1","doi-asserted-by":"publisher","DOI":"10.1021\/bi992505b"},{"key":"e_1_2_8_31_1","doi-asserted-by":"publisher","DOI":"10.1002\/anie.201612495"},{"key":"e_1_2_8_32_1","doi-asserted-by":"publisher","DOI":"10.1039\/D0OB00114G"},{"key":"e_1_2_8_33_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.jmedchem.6b01379"},{"key":"e_1_2_8_34_1","unstructured":"X.Zhou Z.Zhang M. P.Arend W.-B.Ho D.Ng WO 2023\/028341A1."},{"key":"e_1_2_8_35_1","unstructured":"Z. R. D.Cai Z.Ji M.Jin H.Kim C. U.Mish M. R.Phillips B. W.Pyun H.-j X. C.Sheng Q.Wu C. S.Zonte WO 2011\/156610\u2005A2."},{"key":"e_1_2_8_36_1","doi-asserted-by":"publisher","DOI":"10.1002\/ejoc.200300531"}],"container-title":["ChemMedChem"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/chemistry-europe.onlinelibrary.wiley.com\/doi\/pdf\/10.1002\/cmdc.202400901","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2025,10,12]],"date-time":"2025-10-12T21:55:01Z","timestamp":1760306101000},"score":1,"resource":{"primary":{"URL":"https:\/\/chemistry-europe.onlinelibrary.wiley.com\/doi\/10.1002\/cmdc.202400901"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2025,1,14]]},"references-count":36,"journal-issue":{"issue":"7","published-print":{"date-parts":[[2025,4]]}},"alternative-id":["10.1002\/cmdc.202400901"],"URL":"https:\/\/doi.org\/10.1002\/cmdc.202400901","archive":["Portico"],"relation":{},"ISSN":["1860-7179","1860-7187"],"issn-type":[{"value":"1860-7179","type":"print"},{"value":"1860-7187","type":"electronic"}],"subject":[],"published":{"date-parts":[[2025,1,14]]},"assertion":[{"value":"2024-11-11","order":0,"name":"received","label":"Received","group":{"name":"publication_history","label":"Publication History"}},{"value":"2025-01-14","order":3,"name":"published","label":"Published","group":{"name":"publication_history","label":"Publication History"}}],"article-number":"e202400901"}}