{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,6,11]],"date-time":"2026-06-11T17:08:37Z","timestamp":1781197717861,"version":"3.54.1"},"reference-count":49,"publisher":"The Royal Society","issue":"11","license":[{"start":{"date-parts":[[2024,11,1]],"date-time":"2024-11-01T00:00:00Z","timestamp":1730419200000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/creativecommons.org\/licenses\/by\/4.0\/"},{"start":{"date-parts":[[2024,11,1]],"date-time":"2024-11-01T00:00:00Z","timestamp":1730419200000},"content-version":"tdm","delay-in-days":0,"URL":"http:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100004242","name":"Princess Nourah Bint Abdulrahman University","doi-asserted-by":"publisher","id":[{"id":"10.13039\/501100004242","id-type":"DOI","asserted-by":"publisher"}]},{"name":"Researchers Supporting Project"},{"name":"Princess Nourah bint Abdulrahman University, Riyadh, Saudi Arabia"},{"DOI":"10.13039\/501100002383","name":"King Saud University","doi-asserted-by":"publisher","id":[{"id":"10.13039\/501100002383","id-type":"DOI","asserted-by":"publisher"}]},{"name":"King Saud University, Riyadh, Saudi Arabia"}],"content-domain":{"domain":["royalsocietypublishing.org"],"crossmark-restriction":true},"short-container-title":["R. Soc. Open Sci."],"published-print":{"date-parts":[[2024,11]]},"abstract":"<jats:p>\n                    Inflammation is a complex physiological response associated with the onset and progression of various disorders, including diabetes. In this study, we synthesized a series of diclofenac acid derivatives and evaluated their potential anti-diabetic and anti-inflammatory activities. The compounds were specifically assessed for their ability to inhibit 15-lipoxygenase (15-LOX) and \u03b1-glucosidase enzymes. The structures of synthesized derivatives were confirmed through\n                    <jats:sup>1<\/jats:sup>\n                    H nuclear magnetic resonance (NMR),\n                    <jats:sup>13<\/jats:sup>\n                    C-NMR and high-resolution mass spectrometry (electron ionization) analysis. All these synthesized derivatives exhibited varying degrees of inhibitory activity against LOX, when compared with standard drugs, compounds\n                    <jats:bold>5a<\/jats:bold>\n                    (half-maximal inhibitory concentration (IC\n                    <jats:sub>50<\/jats:sub>\n                    ) 14 \u00b1 1 \u00b5M),\n                    <jats:bold>5b<\/jats:bold>\n                    (IC\n                    <jats:sub>50<\/jats:sub>\n                    61 \u00b1 1 \u00b5M) and\n                    <jats:bold>7c<\/jats:bold>\n                    (IC\n                    <jats:sub>50<\/jats:sub>\n                    67 \u00b1 1 \u00b5M) showed good activity against the LOX enzyme. While the \u03b1-glucosidase inhibitory results revealed that most of the compounds exhibited significant activity when compared with the standard drug acarbose (376 \u00b1 1 \u00b5M). The most potent compounds as \u03b1\n                    <jats:bold>-<\/jats:bold>\n                    glucosidase inhibitors were\n                    <jats:bold>7b<\/jats:bold>\n                    (3 \u00b1 1 \u00b5M),\n                    <jats:bold>4b<\/jats:bold>\n                    (5 \u00b1 1 \u00b5M),\n                    <jats:bold>7a<\/jats:bold>\n                    (7 \u00b1 1 \u00b5M) and\n                    <jats:bold>8b<\/jats:bold>\n                    (11 \u00b1 1 \u00b5M). All these active compounds were found to be least toxic and maintained the mononuclear cells viability at 96\u201397% compared with that of controls as determined by multi-transaction translator assay. Molecular docking studies further reiterated the significance of these \u2018lead\u2019 compounds with great potential against the target enzymes in the process of drug discovery.\n                  <\/jats:p>","DOI":"10.1098\/rsos.240543","type":"journal-article","created":{"date-parts":[[2024,11,19]],"date-time":"2024-11-19T19:05:47Z","timestamp":1732043147000},"update-policy":"https:\/\/doi.org\/10.1098\/crossmark-policy","source":"Crossref","is-referenced-by-count":7,"title":["Synthesis and biological evaluation of diclofenac acid derivatives as potential lipoxygenase and \u03b1-glucosidase inhibitors"],"prefix":"10.1098","volume":"11","author":[{"given":"Asma","family":"Sardar","sequence":"first","affiliation":[{"name":"Department of Chemistry, Hazara University, Mansehra 21300, Pakistan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Obaid-ur-Rahman","family":"Abid","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Hazara University, Mansehra 21300, Pakistan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0128-0377","authenticated-orcid":true,"given":"Wajid","family":"Rehman","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Hazara University, Mansehra 21300, Pakistan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Liaqat","family":"Rasheed","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Hazara University, Mansehra 21300, Pakistan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-0483-8113","authenticated-orcid":true,"given":"Mohammed M.","family":"Alanazi","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Saima","family":"Daud","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Hazara University, Mansehra 21300, Pakistan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Muhammad","family":"Rafiq","sequence":"additional","affiliation":[{"name":"South China University of Technology School of Chemistry and Chemical Engineering, Guangzhou, People\u2019s Republic of China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-3415-9277","authenticated-orcid":true,"given":"Abdul","family":"Wadood","sequence":"additional","affiliation":[{"name":"Department of Biochemistry, Abdul Wali Khan University, Mardan, Khyber Pakhtunkhwa, Pakistan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Muhammed","family":"Shakeel","sequence":"additional","affiliation":[{"name":"State Key Laboratory of Chemical Resource Engineering, Beijing University of Chemical Technology, Beijing 100029, People\u2019s Republic of China"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"175","published-online":{"date-parts":[[2024,11,20]]},"reference":[{"key":"e_1_3_8_2_2","article-title":"Diabetes mellitus and prevalence of other comorbid conditions: a systematic review","volume":"15","author":"Bodke H","year":"2023","unstructured":"Bodke H, Wagh V, Kakar G. 2023 Diabetes mellitus and prevalence of other comorbid conditions: a systematic review. Cureus 15, e49374. (doi:10.7759\/cureus.49374)","journal-title":"Cureus"},{"key":"e_1_3_8_3_2","doi-asserted-by":"publisher","DOI":"10.1007\/s11655-023-3598-z"},{"key":"e_1_3_8_4_2","doi-asserted-by":"publisher","DOI":"10.1097\/MD.0000000000035391"},{"key":"e_1_3_8_5_2","doi-asserted-by":"publisher","DOI":"10.3390\/ijms21176275"},{"key":"e_1_3_8_6_2","doi-asserted-by":"publisher","DOI":"10.1021\/acs.joc.3c01315"},{"key":"e_1_3_8_7_2","doi-asserted-by":"publisher","DOI":"10.1002\/cjoc.202200406"},{"key":"e_1_3_8_8_2","doi-asserted-by":"publisher","DOI":"10.3390\/ijms20143393"},{"key":"e_1_3_8_9_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.arabjc.2022.104300"},{"key":"e_1_3_8_10_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.jcis.2022.04.077"},{"key":"e_1_3_8_11_2","doi-asserted-by":"publisher","DOI":"10.1002\/advs.202205604"},{"key":"e_1_3_8_12_2","doi-asserted-by":"publisher","DOI":"10.3906\/kim-1706-50"},{"key":"e_1_3_8_13_2","doi-asserted-by":"publisher","DOI":"10.3390\/ijms23031923"},{"key":"e_1_3_8_14_2","doi-asserted-by":"publisher","DOI":"10.1002\/adma.202206594"},{"key":"e_1_3_8_15_2","first-page":"1632","article-title":"Novel oxadiazole derivatives as potent inhibitors of \u03b1-amylase and \u03b1-glucosidase enzymes: synthesis, in vitro evaluation, and molecular docking studies","volume":"24","author":"Bukhari A","year":"2021","unstructured":"Bukhari A, Nadeem H, Imran M, Muhammad SA. 2021 Novel oxadiazole derivatives as potent inhibitors of \u03b1-amylase and \u03b1-glucosidase enzymes: synthesis, in vitro evaluation, and molecular docking studies. Iran. J. Basic Med. Sci. 24, 1632\u20131642. (doi:10.22038\/IJBMS.2021.58429.12977)","journal-title":"Iran. J. Basic Med. Sci."},{"key":"e_1_3_8_16_2","doi-asserted-by":"publisher","DOI":"10.3892\/ijmm.2017.2989"},{"key":"e_1_3_8_17_2","doi-asserted-by":"publisher","DOI":"10.1038\/s41467-022-31997-8"},{"key":"e_1_3_8_18_2","doi-asserted-by":"publisher","DOI":"10.3390\/ijms25168638"},{"key":"e_1_3_8_19_2","doi-asserted-by":"publisher","DOI":"10.1111\/dme.15031"},{"key":"e_1_3_8_20_2","doi-asserted-by":"publisher","DOI":"10.3389\/fendo.2022.1085092"},{"key":"e_1_3_8_21_2","doi-asserted-by":"publisher","DOI":"10.1177\/14791641231173627"},{"key":"e_1_3_8_22_2","doi-asserted-by":"publisher","DOI":"10.1111\/dme.15031"},{"key":"e_1_3_8_23_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.bioorg.2019.03.076"},{"key":"e_1_3_8_24_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.ijbiomac.2024.132196"},{"key":"e_1_3_8_25_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.pneurobio.2022.102280"},{"key":"e_1_3_8_26_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.molstruc.2024.137712"},{"key":"e_1_3_8_27_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.carbpol.2013.01.045"},{"key":"e_1_3_8_28_2","doi-asserted-by":"publisher","DOI":"10.1039\/D3FO05456J"},{"key":"e_1_3_8_29_2","doi-asserted-by":"publisher","DOI":"10.2174\/1871523018666190514112048"},{"key":"e_1_3_8_30_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.phrs.2023.106954"},{"key":"e_1_3_8_31_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.foodhyd.2022.107503"},{"key":"e_1_3_8_32_2","doi-asserted-by":"publisher","DOI":"10.1002\/ddr.22051"},{"key":"e_1_3_8_33_2","doi-asserted-by":"publisher","DOI":"10.3389\/fbioe.2022.940511"},{"key":"e_1_3_8_34_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.ajem.2020.11.022"},{"key":"e_1_3_8_35_2","doi-asserted-by":"publisher","DOI":"10.1186\/s12951-022-01715-z"},{"key":"e_1_3_8_36_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.giec.2006.01.001"},{"key":"e_1_3_8_37_2","doi-asserted-by":"publisher","DOI":"10.2174\/1874104501711010146"},{"key":"e_1_3_8_38_2","doi-asserted-by":"publisher","DOI":"10.3390\/ph7040453"},{"key":"e_1_3_8_39_2","first-page":"145","article-title":"Amide prodrugs of NSAIDs: synthesis and biological evaluation with a hydrolysis study","volume":"4","author":"Husain A","year":"2015","unstructured":"Husain A, Ahuja P, Ahmad A, Khan A. 2015 Amide prodrugs of NSAIDs: synthesis and biological evaluation with a hydrolysis study. Acad. J. Pharm. 4, 145\u2013152.","journal-title":"Acad. J. Pharm."},{"key":"e_1_3_8_40_2","first-page":"116932","article-title":"Recent advances in droplet microfluidics for single-cell analysis","volume":"159","author":"Jiang Z","year":"2023","unstructured":"Jiang Z, Shi H, Tang X, Qin J. 2023 Recent advances in droplet microfluidics for single-cell analysis. TrAC. 159, 116932. (doi:10.1016\/j.trac.2023.116932)","journal-title":"TrAC."},{"key":"e_1_3_8_41_2","first-page":"59","article-title":"Synthesis, hydrolysis studies and pharmacodynamic profile of novelcolon-specific mutual prodrug of aceclofenac with amino acids","volume":"1","author":"Rasheed A","year":"2009","unstructured":"Rasheed A, Theja I, Kumar A, Lvanya Y, Royal PR, Krishna SV. 2009 Synthesis, hydrolysis studies and pharmacodynamic profile of novelcolon-specific mutual prodrug of aceclofenac with amino acids. Der. Pharm. Chem. 1, 59\u201371.","journal-title":"Der. Pharm. Chem."},{"key":"e_1_3_8_42_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.joto.2022.09.002"},{"key":"e_1_3_8_43_2","first-page":"555642","article-title":"Synthesis, characterization & biological evaluation of mutual prodrugs of some selected NSAIDs conjugated with different antioxidant via different amino acids","volume":"4","author":"Sharma N","year":"2017","unstructured":"Sharma N. 2017 Synthesis, characterization & biological evaluation of mutual prodrugs of some selected NSAIDs conjugated with different antioxidant via different amino acids. Org. Med. Chem. Int. J. 4, 555642. (doi:10.19080\/OMCIJ.2017.04.555642)","journal-title":"Org. Med. Chem. Int. J."},{"key":"e_1_3_8_44_2","doi-asserted-by":"publisher","DOI":"10.3390\/ijms22105067"},{"key":"e_1_3_8_45_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.heliyon.2024.e27371"},{"key":"e_1_3_8_46_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.bioorg.2020.104499"},{"key":"e_1_3_8_47_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.heliyon.2024.e27303"},{"key":"e_1_3_8_48_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.jscs.2013.05.001"},{"key":"e_1_3_8_49_2","doi-asserted-by":"publisher","DOI":"10.5267\/j.ccl.2022.12.004"},{"key":"e_1_3_8_50_2","author":"Sardar A","year":"2024","unstructured":"Sardar A, AbidOR, Rehman W, Rasheed L et al. 2024. Supplementary material from: Synthesis and biological evaluation of diclofenac acid derivatives as potential lipoxygenase and \u03b1-glucosidase inhibitors. FigShare (doi:10.6084\/m9.figshare.c.7539177)","journal-title":"Supplementary material from: Synthesis and biological evaluation of diclofenac acid derivatives as potential lipoxygenase and \u03b1-glucosidase inhibitors. FigShare"}],"container-title":["Royal Society Open Science"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/royalsocietypublishing.org\/doi\/pdf\/10.1098\/rsos.240543","content-type":"application\/pdf","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/royalsocietypublishing.org\/doi\/full-xml\/10.1098\/rsos.240543","content-type":"application\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/royalsocietypublishing.org\/doi\/pdf\/10.1098\/rsos.240543","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2024,11,19]],"date-time":"2024-11-19T19:06:33Z","timestamp":1732043193000},"score":1,"resource":{"primary":{"URL":"https:\/\/royalsocietypublishing.org\/doi\/10.1098\/rsos.240543"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2024,11]]},"references-count":49,"journal-issue":{"issue":"11","published-print":{"date-parts":[[2024,11]]}},"alternative-id":["10.1098\/rsos.240543"],"URL":"https:\/\/doi.org\/10.1098\/rsos.240543","relation":{"has-review":[{"id-type":"doi","id":"10.1098\/RSOS.240543\/v1\/review2","asserted-by":"object"},{"id-type":"doi","id":"10.1098\/RSOS.240543\/v1\/review1","asserted-by":"object"},{"id-type":"doi","id":"10.1098\/RSOS.240543\/v2\/response1","asserted-by":"object"},{"id-type":"doi","id":"10.1098\/RSOS.240543\/v3\/decision1","asserted-by":"object"},{"id-type":"doi","id":"10.1098\/RSOS.240543\/v2\/decision1","asserted-by":"object"},{"id-type":"doi","id":"10.1098\/RSOS.240543\/v1\/review3","asserted-by":"object"},{"id-type":"doi","id":"10.1098\/RSOS.240543\/v4\/decision1","asserted-by":"object"},{"id-type":"doi","id":"10.1098\/RSOS.240543\/v1\/decision1","asserted-by":"object"},{"id-type":"doi","id":"10.1098\/RSOS.240543\/v3\/review3","asserted-by":"object"},{"id-type":"doi","id":"10.1098\/RSOS.240543\/v3\/review2","asserted-by":"object"},{"id-type":"doi","id":"10.1098\/RSOS.240543\/v4\/response1","asserted-by":"object"},{"id-type":"doi","id":"10.1098\/RSOS.240543\/v3\/review1","asserted-by":"object"},{"id-type":"doi","id":"10.1098\/RSOS.240543\/v3\/response1","asserted-by":"object"}]},"ISSN":["2054-5703"],"issn-type":[{"value":"2054-5703","type":"electronic"}],"subject":[],"published":{"date-parts":[[2024,11]]},"assertion":[{"value":"2024-04-17","order":0,"name":"received","label":"Received","group":{"name":"publication_history","label":"Publication History"}},{"value":"2024-05-25","order":1,"name":"revised","label":"Revised","group":{"name":"publication_history","label":"Publication History"}},{"value":"2024-09-17","order":2,"name":"accepted","label":"Accepted","group":{"name":"publication_history","label":"Publication History"}},{"value":"2024-11-20","order":3,"name":"published","label":"Published","group":{"name":"publication_history","label":"Publication History"}}],"article-number":"240543"}}