{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,29]],"date-time":"2026-09-29T15:02:10Z","timestamp":1790694130893,"version":"4.1.0"},"reference-count":62,"publisher":"Wiley","issue":"8","license":[{"start":{"date-parts":[[2023,5,26]],"date-time":"2023-05-26T00:00:00Z","timestamp":1685059200000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"},{"start":{"date-parts":[[2023,5,26]],"date-time":"2023-05-26T00:00:00Z","timestamp":1685059200000},"content-version":"tdm","delay-in-days":0,"URL":"http:\/\/doi.wiley.com\/10.1002\/tdm_license_1.1"}],"content-domain":{"domain":["onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["Archiv der Pharmazie"],"published-print":{"date-parts":[[2023,8]]},"abstract":"<jats:title>Abstract<\/jats:title>\n                  <jats:p>\n                    \u03b1\u2010Glucosidase inhibition is widely used in the oral management of diabetes mellitus (DM), a disease characterized by high blood sugar levels (hyperglycemia) and abnormal carbohydrate metabolism. In this respect, a series of 1,2,3\u2010triazole\u20101,3,4\u2010thiadiazole hybrids\n                    <jats:bold>7a\u2013j<\/jats:bold>\n                    were synthesized, inspired by a copper\u2010catalyzed one\u2010pot azidation\/click assembly approach. All the synthesized hybrids were screened for inhibition of the \u03b1\u2010glucosidase enzyme, displaying IC\n                    <jats:sub>50<\/jats:sub>\n                    values ranging from 63.35\u2009\u00b1\u20090.72 to 613.57\u2009\u00b1\u20091.98\u2009\u03bcM, as compared to acarbose (reference) with IC\n                    <jats:sub>50<\/jats:sub>\n                    of 844.81\u2009\u00b1\u20090.53\u2009\u03bcM. The hybrids\n                    <jats:bold>7h<\/jats:bold>\n                    and\n                    <jats:bold>7e<\/jats:bold>\n                    with 3\u2010nitro and 4\u2010methoxy substituents at the phenyl ring of the thiadiazole moiety were the best active hybrids of this series with IC\n                    <jats:sub>50<\/jats:sub>\n                    values of 63.35\u2009\u00b1\u20090.72\u2009\u03bcM, and 67.61\u2009\u00b1\u20090.64\u2009\u03bcM, respectively. Enzyme kinetics analysis of these compounds revealed a mixed mode of inhibition. Moreover, molecular docking studies were also performed to gain insights into the structure\u2013activity\u2010relationships of the potent compounds and their corresponding analogs.\n                  <\/jats:p>","DOI":"10.1002\/ardp.202300145","type":"journal-article","created":{"date-parts":[[2023,5,26]],"date-time":"2023-05-26T18:20:13Z","timestamp":1685125213000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":4,"title":["Synthesis of 1,2,3\u2010triazole\u20101,3,4\u2010thiadiazole hybrids as novel \u03b1\u2010glucosidase inhibitors by in situ azidation\/click assembly"],"prefix":"10.1002","volume":"356","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-1008-7328","authenticated-orcid":false,"given":"Hariom","family":"Kumar","sequence":"first","affiliation":[{"name":"Department of Chemistry Babasaheb Bhimrao Ambedkar University Lucknow Uttar Pradesh India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-1679-0890","authenticated-orcid":false,"given":"Manoj","family":"Dhameja","sequence":"additional","affiliation":[{"name":"Department of Chemistry Babasaheb Bhimrao Ambedkar University Lucknow Uttar Pradesh India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sirisha","family":"Kurella","sequence":"additional","affiliation":[{"name":"Institute of Science and Technology Jawaharlal Nehru Technological University Kukatpally, Hyderabad Telangana India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Adepally","family":"Uma","sequence":"additional","affiliation":[{"name":"Institute of Science and Technology Jawaharlal Nehru Technological University Kukatpally, Hyderabad Telangana India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-7133-1873","authenticated-orcid":false,"given":"Preeti","family":"Gupta","sequence":"additional","affiliation":[{"name":"Department of Chemistry Babasaheb Bhimrao Ambedkar University Lucknow Uttar Pradesh India"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2023,5,26]]},"reference":[{"key":"e_1_2_7_2_1","doi-asserted-by":"publisher","DOI":"10.1016\/S2213-8587(13)70112-8"},{"key":"e_1_2_7_3_1","doi-asserted-by":"publisher","DOI":"10.1038\/485S2a"},{"key":"e_1_2_7_4_1","doi-asserted-by":"publisher","DOI":"10.1371\/journal.pone.0079324"},{"key":"e_1_2_7_5_1","doi-asserted-by":"publisher","DOI":"10.4103\/2468-8827.184853"},{"key":"e_1_2_7_6_1","doi-asserted-by":"publisher","DOI":"10.1038\/nrneph.2018.9"},{"key":"e_1_2_7_7_1","doi-asserted-by":"publisher","DOI":"10.1038\/ncpendmet0638"},{"key":"e_1_2_7_8_1","unstructured":"https:\/\/www.who.int\/health-topics\/diabetes#tab=tab_1(accessed: September 2022)."},{"key":"e_1_2_7_9_1","unstructured":"www.idf.org(assessed: September 2022)."},{"key":"e_1_2_7_10_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2018.04.061"},{"key":"e_1_2_7_11_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2015.08.043"},{"key":"e_1_2_7_12_1","doi-asserted-by":"publisher","DOI":"10.1371\/journal.pntd.0004524"},{"key":"e_1_2_7_13_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.tetasy.2015.05.008"},{"key":"e_1_2_7_14_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bioorg.2016.08.011"},{"key":"e_1_2_7_15_1","doi-asserted-by":"publisher","DOI":"10.1002\/aoc.4725"},{"key":"e_1_2_7_16_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.molstruc.2019.07.039"},{"key":"e_1_2_7_17_1","doi-asserted-by":"publisher","DOI":"10.1039\/D2RA03307K"},{"key":"e_1_2_7_18_1","doi-asserted-by":"publisher","DOI":"10.1038\/s41598-023-28828-1"},{"key":"e_1_2_7_19_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2019.04.025"},{"key":"e_1_2_7_20_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.molstruc.2022.132469"},{"key":"e_1_2_7_21_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2023.115119"},{"key":"e_1_2_7_22_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bioorg.2020.104082"},{"key":"e_1_2_7_23_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.molstruc.2023.135115"},{"key":"e_1_2_7_24_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bioorg.2021.105423"},{"key":"e_1_2_7_25_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ijbiomac.2020.11.170"},{"key":"e_1_2_7_26_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ijbiomac.2020.10.263"},{"key":"e_1_2_7_27_1","first-page":"68","volume":"6","author":"Lihumis H. S.","year":"2022","journal-title":"Asian J. Green Chem"},{"key":"e_1_2_7_28_1","doi-asserted-by":"publisher","DOI":"10.3390\/molecules25092015"},{"key":"e_1_2_7_29_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.chemrev.5b00408"},{"key":"e_1_2_7_30_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.chemrev.0c00920"},{"key":"e_1_2_7_31_1","doi-asserted-by":"publisher","DOI":"10.1002\/ajoc.202000021"},{"key":"e_1_2_7_32_1","volume":"6","author":"Kumar H.","year":"2021","journal-title":"Chem. Select"},{"key":"e_1_2_7_33_1","doi-asserted-by":"publisher","DOI":"10.3389\/fchem.2022.891484"},{"key":"e_1_2_7_34_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.catcom.2023.106629"},{"key":"e_1_2_7_35_1","doi-asserted-by":"publisher","DOI":"10.1039\/C5CY01847A"},{"key":"e_1_2_7_36_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bioorg.2017.01.010"},{"key":"e_1_2_7_37_1","doi-asserted-by":"publisher","DOI":"10.2174\/1568026616666160824104655"},{"key":"e_1_2_7_38_1","doi-asserted-by":"publisher","DOI":"10.2174\/1568026621666210913122828"},{"key":"e_1_2_7_39_1","doi-asserted-by":"publisher","DOI":"10.2174\/1568026621666210303145759"},{"key":"e_1_2_7_40_1","doi-asserted-by":"publisher","DOI":"10.2174\/1871520616666160811113531"},{"key":"e_1_2_7_41_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2022.114454"},{"key":"e_1_2_7_42_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2019.02.055"},{"key":"e_1_2_7_43_1","doi-asserted-by":"publisher","DOI":"10.1021\/cr400131u"},{"key":"e_1_2_7_44_1","doi-asserted-by":"publisher","DOI":"10.3390\/chemistry4040107"},{"key":"e_1_2_7_45_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.medidd.2022.100150"},{"key":"e_1_2_7_46_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bioorg.2021.105210"},{"key":"e_1_2_7_47_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ijbiomac.2021.12.147"},{"key":"e_1_2_7_48_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bioorg.2018.03.022"},{"key":"e_1_2_7_49_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bmcl.2021.128447"},{"key":"e_1_2_7_50_1","doi-asserted-by":"publisher","DOI":"10.1111\/cbdd.12125"},{"key":"e_1_2_7_51_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2014.12.035"},{"key":"e_1_2_7_52_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.cgd.9b01060"},{"key":"e_1_2_7_53_1","doi-asserted-by":"publisher","DOI":"10.1080\/13543776.2017.1272575"},{"key":"e_1_2_7_54_1","doi-asserted-by":"publisher","DOI":"10.4155\/fmc-2022-0289"},{"key":"e_1_2_7_55_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.molstruc.2022.134339"},{"key":"e_1_2_7_56_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bioorg.2022.106028"},{"key":"e_1_2_7_57_1","doi-asserted-by":"publisher","DOI":"10.1021\/ol501618z"},{"key":"e_1_2_7_58_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1742-4658.2010.07810.x"},{"key":"e_1_2_7_59_1","doi-asserted-by":"publisher","DOI":"10.1155\/2013\/527570"},{"key":"e_1_2_7_60_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2020.112034"},{"key":"e_1_2_7_61_1","doi-asserted-by":"publisher","DOI":"10.1002\/jcc.21256"},{"key":"e_1_2_7_62_1","doi-asserted-by":"publisher","DOI":"10.1021\/acsomega.7b01299"},{"key":"e_1_2_7_63_1","unstructured":"BIOVIA Dassault Syst\u00e8mes Discovery Studio Visualizer v20.1.0.19295 San Diego: Dassault Syst\u00e8mes 2020."}],"container-title":["Archiv der Pharmazie"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/onlinelibrary.wiley.com\/doi\/pdf\/10.1002\/ardp.202300145","content-type":"application\/pdf","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/onlinelibrary.wiley.com\/doi\/full-xml\/10.1002\/ardp.202300145","content-type":"application\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/onlinelibrary.wiley.com\/doi\/pdf\/10.1002\/ardp.202300145","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2026,9,29]],"date-time":"2026-09-29T14:46:03Z","timestamp":1790693163000},"score":1,"resource":{"primary":{"URL":"https:\/\/onlinelibrary.wiley.com\/doi\/10.1002\/ardp.202300145"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2023,5,26]]},"references-count":62,"journal-issue":{"issue":"8","published-print":{"date-parts":[[2023,8]]}},"alternative-id":["10.1002\/ardp.202300145"],"URL":"https:\/\/doi.org\/10.1002\/ardp.202300145","archive":["Portico"],"relation":{},"ISSN":["0365-6233","1521-4184"],"issn-type":[{"value":"0365-6233","type":"print"},{"value":"1521-4184","type":"electronic"}],"subject":[],"published":{"date-parts":[[2023,5,26]]},"assertion":[{"value":"2023-03-13","order":0,"name":"received","label":"Received","group":{"name":"publication_history","label":"Publication History"}},{"value":"2023-05-02","order":2,"name":"accepted","label":"Accepted","group":{"name":"publication_history","label":"Publication History"}},{"value":"2023-05-26","order":3,"name":"published","label":"Published","group":{"name":"publication_history","label":"Publication History"}}],"article-number":"2300145"}}