{"data":{"id":"10.6084/m9.figshare.c.2030252","type":"dois","attributes":{"doi":"10.6084/m9.figshare.c.2030252","prefix":"10.6084","suffix":"m9.figshare.c.2030252","identifiers":[],"alternateIdentifiers":[],"creators":[{"name":"Huang, Guoli","givenName":"Guoli","familyName":"Huang","affiliation":[],"nameIdentifiers":[]},{"name":"Feng, Li","givenName":"Li","familyName":"Feng","affiliation":[],"nameIdentifiers":[]},{"name":"Liu, Bo","givenName":"Bo","familyName":"Liu","affiliation":[],"nameIdentifiers":[]},{"name":"He, Yi","givenName":"Yi","familyName":"He","affiliation":[],"nameIdentifiers":[]},{"name":"Li, Yiming","givenName":"Yiming","familyName":"Li","affiliation":[],"nameIdentifiers":[]},{"name":"Chen, Yegao","givenName":"Yegao","familyName":"Chen","affiliation":[],"nameIdentifiers":[]}],"titles":[{"title":"Synthesis and biological evaluation of nigranoic acid esters as novel human neutrophil elastase inhibitors"}],"publisher":"Taylor \u0026 Francis","container":{},"publicationYear":2015,"subjects":[{"subject":"Hematology"},{"subject":"Biological Sciences"},{"subject":"Immunology"},{"subject":"FOS: Clinical medicine","schemeUri":"http://www.oecd.org/science/inno/38235147.pdf","subjectScheme":"Fields of Science and Technology (FOS)"},{"subject":"Ecology"},{"subject":"FOS: Biological sciences","schemeUri":"http://www.oecd.org/science/inno/38235147.pdf","subjectScheme":"Fields of Science and Technology (FOS)"},{"subject":"Chemistry"},{"subject":"Earth and Environmental Sciences"},{"subject":"Biotechnology"},{"subject":"Pharmacology"},{"subject":"Physiology"},{"subject":"Neuroscience"},{"subject":"Microbiology"},{"subject":"Biochemistry"}],"contributors":[],"dates":[{"date":"2015-12-05","dateType":"Created"},{"date":"2019-08-19","dateType":"Updated"},{"date":"2015","dateType":"Issued"}],"language":null,"types":{"ris":"GEN","bibtex":"misc","citeproc":"article","schemaOrg":"Collection","resourceType":"Collection","resourceTypeGeneral":"Collection"},"relatedIdentifiers":[],"relatedItems":[],"sizes":[],"formats":[],"version":null,"rightsList":[{"rights":"Creative Commons Attribution 4.0 International","rightsUri":"https://creativecommons.org/licenses/by/4.0/legalcode","schemeUri":"https://spdx.org/licenses/","rightsIdentifier":"cc-by-4.0","rightsIdentifierScheme":"SPDX"}],"descriptions":[{"description":"Human neutrophil elastase (HNE) has been implicated as a major contributor in the pathogenesis of diseases, such as lung disorders and other inflammatory diseases. A series of 12 new nigranoic acid esters were regioselectively synthesised in good yields and evaluated for HNE inhibitory activity. Nigranoic acid exhibited significant inhibitory activity against HNE with the IC\u003csub\u003e50\u003c/sub\u003e value of 3.77 μM, and six esters displayed considerable inhibitory effects on HNE with IC\u003csub\u003e50\u003c/sub\u003e values in the range of 2.61–8.95 μM. The nigranoic acid esters having phenyls substituted with bromine and trimethoxyls (\u003cb\u003e3h\u003c/b\u003e and \u003cb\u003e3b\u003c/b\u003e) showed stronger inhibitory activity on HNE than nigranoic acid.","descriptionType":"Abstract"}],"geoLocations":[],"fundingReferences":[],"xml":"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","url":"https://tandf.figshare.com/collections/Synthesis_and_biological_evaluation_of_nigranoic_acid_esters_as_novel_human_neutrophil_elastase_inhibitors/2030252","contentUrl":null,"metadataVersion":2,"schemaVersion":"http://datacite.org/schema/kernel-4","source":"mds","isActive":true,"state":"findable","reason":null,"viewCount":0,"viewsOverTime":[],"downloadCount":0,"downloadsOverTime":[],"referenceCount":0,"citationCount":0,"citationsOverTime":[],"partCount":0,"partOfCount":0,"versionCount":0,"versionOfCount":0,"created":"2015-12-05T17:06:25.000Z","registered":"2015-12-05T17:06:26.000Z","published":"2015","updated":"2024-03-21T08:35:01.000Z"},"relationships":{"client":{"data":{"id":"figshare.ars","type":"clients"}},"provider":{"d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