{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,11,1]],"date-time":"2026-11-01T04:15:07Z","timestamp":1793506507115,"version":"4.5.0"},"reference-count":91,"publisher":"MDPI AG","issue":"1","license":[{"start":{"date-parts":[[2022,1,17]],"date-time":"2022-01-17T00:00:00Z","timestamp":1642377600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100004681","name":"Higher Education Commission","doi-asserted-by":"publisher","award":["NRPU"],"award-info":[{"award-number":["NRPU"]}],"id":[{"id":"10.13039\/501100004681","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Pharmaceuticals"],"abstract":"<jats:p>Diabetes mellitus (DM), a complicated metabolic disorder, is due to insensitivity to insulin function or reduction in insulin secretion, which results in postprandial hyperglycemia. \u03b1-Glucosidase inhibitors (AGIs) and \u03b1-amylase inhibitors (AAIs) block the function of digestive enzymes, which delays the carbohydrate hydrolysis process and ultimately helps to control the postprandial hyperglycemia. Diversified 2-(3-(3-methoxybenzoyl)-4-hydroxy-1,1-dioxido-2H-benzo[e][1,2]thiazin-2-yl)-N-arylacetamides were synthesized and evaluated for their in vitro inhibitory potential against \u03b1-glucosidase and \u03b1-amylase enzymes. The compounds with chloro, bromo and methyl substituents demonstrated good inhibition of \u03b1-glucosidase enzymes having IC50 values in the range of 25.88\u201346.25 \u03bcM, which are less than the standard drug, acarbose (IC50 = 58.8 \u03bcM). Similarly, some derivatives having chloro, bromo and nitro substituents were observed potent inhibitors of \u03b1-amylase enzyme, with IC50 values of 7.52 to 15.06 \u03bcM, lower than acarbose (IC50 = 17.0 \u03bcM). In addition, the most potent compound, N-(4-bromophenyl)-2-(4-hydroxy-3-(3-methoxybenzoyl)-1,1-dioxido-2H-benzo[e][1,2]thiazin-2-yl)acetamide (12i), was found to be a non-competitive and competitive inhibitor of \u03b1-glucosidase and \u03b1-amylase enzymes, respectively, during kinetic studies. The molecular docking studies provided the binding modes of active compounds and the molecular dynamics simulation studies of compound 12i in complex with \u03b1-amylase also showed that the compound is binding in a fashion similar to that predicted by molecular docking studies.<\/jats:p>","DOI":"10.3390\/ph15010106","type":"journal-article","created":{"date-parts":[[2022,1,17]],"date-time":"2022-01-17T20:46:03Z","timestamp":1642452363000},"page":"106","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":42,"title":["Identification of Cyclic Sulfonamides with an N-Arylacetamide Group as \u03b1-Glucosidase and \u03b1-Amylase Inhibitors: Biological Evaluation and Molecular Modeling"],"prefix":"10.3390","volume":"15","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-8565-4024","authenticated-orcid":false,"given":"Furqan Ahmad","family":"Saddique","sequence":"first","affiliation":[{"name":"Department of Chemistry, Government College University, Faisalabad 38000, Pakistan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-1302-8056","authenticated-orcid":false,"given":"Matloob","family":"Ahmad","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Government College University, Faisalabad 38000, Pakistan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-5495-805X","authenticated-orcid":false,"given":"Usman Ali","family":"Ashfaq","sequence":"additional","affiliation":[{"name":"Department of Bioinformatics and Biotechnology, Government College University, Faisalabad 38000, Pakistan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Muhammad","family":"Muddassar","sequence":"additional","affiliation":[{"name":"Department of Biosciences, COMSATS University Islamabad, Park Road, Islamabad 45500, Pakistan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sadia","family":"Sultan","sequence":"additional","affiliation":[{"name":"Faculty of Pharmacy, Puncak Alam Campus, Universiti Teknologi MARA, Bandar Puncak Alam 42300, Selangor Darul Ehsan, Malaysia"},{"name":"Atta-ur-Rahman Institute for Natural Products Discovery (AuRIns), Puncak Alam Campus, Universiti Teknologi MARA, Bandar Puncak Alam 42300, Selangor Darul Ehsan, Malaysia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Magdi E. 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