{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,20]],"date-time":"2025-10-20T18:45:36Z","timestamp":1760985936965,"version":"3.40.5"},"reference-count":0,"publisher":"Bentham Science Publishers Ltd.","issue":"1","content-domain":{"domain":["eurekaselect.com"],"crossmark-restriction":true},"short-container-title":["CAD"],"published-print":{"date-parts":[[2022,2]]},"abstract":"<jats:sec>\n<jats:title>Background:<\/jats:title>\n<jats:p>Diabetes mellitus is a chronic metabolic disorder, characterized by hyperglycemia over a\nprolonged period, disturbance of fat, protein and carbohydrate metabolism, resulting from defective insulin secretion,\ninsulin action or both. Dipeptidyl peptidase-IV (DPP-IV) inhibitors are relatively a new class of oral hypoglycemic agents\nthat reduces the deterioration of gut-derived endogenous incretin hormones that are secreted in response to food ingestion\nto stimulate the secretion of insulin from beta cells of pancreas.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Objective:<\/jats:title>\n<jats:p> In this study, synthesis, characterization, and biological assessment of twelve novel phenanthridine\nsulfonamide derivatives 3a-3l as potential DPP-IV inhibitors was carried out. The target compounds were docked to study\nthe molecular interactions and binding affinities against DPP-IV enzyme.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Methods:<\/jats:title>\n<jats:p> The synthesized molecules were characterized using 1H-NMR, 13C-NMR, IR, and MS. Quantum-polarized\nligand docking (QPLD) was also performed.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Results:<\/jats:title>\n<jats:p> In vitro biological evaluation of compounds 3a-3l reveals comparable DPP-IV inhibitory activities ranging from\n10%-46% at 100 \u00b5M concentration, where compound 3d harboring ortho-fluoro moiety exhibited the highest inhibitory\nactivity. QPLD study shows that compounds 3a-3l accommodate DPP-IV binding site and form H-bonding with the R125,\nE205, E206, S209, F357, R358, K554, W629, S630, Y631, Y662, R669 and Y752 backbones.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Conclusion:<\/jats:title>\n<jats:p> In conclusion, phenanthridine sulfonamides could serve as potential DPP-IV inhibitors that require further\nstructural optimization in order to enhance their inhibitory activity.<\/jats:p>\n<\/jats:sec>","DOI":"10.2174\/1573409916666201007124122","type":"journal-article","created":{"date-parts":[[2020,10,8]],"date-time":"2020-10-08T09:18:43Z","timestamp":1602148723000},"page":"9-25","update-policy":"https:\/\/doi.org\/10.2174\/bsp_crossmark_policy","source":"Crossref","is-referenced-by-count":7,"title":["Phenanthridine Sulfonamide Derivatives as Potential DPP-IV Inhibitors:\nDesign, Synthesis and Biological Evaluation"],"prefix":"10.2174","volume":"18","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-7797-8918","authenticated-orcid":true,"given":"Reema Abu","family":"Khalaf","sequence":"first","affiliation":[{"name":"Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman,Jordan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Shorooq","family":"Alqazaqi","sequence":"additional","affiliation":[{"name":"Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman,Jordan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Maram","family":"Aburezeq","sequence":"additional","affiliation":[{"name":"Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman,Jordan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Dima","family":"Sabbah","sequence":"additional","affiliation":[{"name":"Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman,Jordan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ghadeer","family":"Albadawi","sequence":"additional","affiliation":[{"name":"Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman,Jordan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ghassan Abu","family":"Sheikha","sequence":"additional","affiliation":[{"name":"Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman,Jordan"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"965","container-title":["Current Computer-Aided Drug Design"],"original-title":[],"language":"en","link":[{"URL":"http:\/\/eurekaselect.com\/article\/download\/186712","content-type":"application\/pdf","content-version":"vor","intended-application":"text-mining"},{"URL":"http:\/\/www.eurekaselect.com\/186712\/article","content-type":"text\/html","content-version":"vor","intended-application":"text-mining"},{"URL":"http:\/\/eurekaselect.com\/article\/download\/186712","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2022,1,19]],"date-time":"2022-01-19T10:00:43Z","timestamp":1642586443000},"score":1,"resource":{"primary":{"URL":"http:\/\/www.eurekaselect.com\/186712\/article"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2022,2]]},"references-count":0,"journal-issue":{"issue":"1","published-print":{"date-parts":[[2022,2]]}},"alternative-id":["LiveAll1"],"URL":"https:\/\/doi.org\/10.2174\/1573409916666201007124122","relation":{},"ISSN":["1573-4099"],"issn-type":[{"type":"print","value":"1573-4099"}],"subject":[],"published":{"date-parts":[[2022,2]]},"assertion":[{"value":"Peer Reviewed","order":0,"name":"review_status","label":"Review Status","group":{"name":"peer_review_details","label":"Peer Review Details"}},{"value":"Single blind","order":1,"name":"review_process","label":"Review Process","group":{"name":"peer_review_details","label":"Peer Review Details"}},{"value":"Checked with iThenticate","order":0,"name":"screening_status","label":"Screening Status","group":{"name":"plagiarism_screening","label":"Plagiarism Screening"}},{"value":"2020-04-12","order":0,"name":"received","label":"Received","group":{"name":"publication_history","label":"Publication History"}},{"value":"2020-09-01","order":1,"name":"revised","label":"Revised","group":{"name":"publication_history","label":"Publication History"}},{"value":"2020-09-03","order":2,"name":"accepted","label":"Accepted","group":{"name":"publication_history","label":"Publication History"}},{"value":"2021-12-30","order":3,"name":"published","label":"Published","group":{"name":"publication_history","label":"Publication History"}}]}}