{"id":{"repo_id":"venda","oai_identifier":"oai:univendspace.univen.ac.za:11602/3190"},"canonical_url":"https://search.dev.ndltd.org/etd/venda/oai:univendspace.univen.ac.za:11602/3190","repository":{"repo_id":"venda","name":"University of Venda","base_url":"https://univendspace.univen.ac.za/server/oai/request"},"display":{"title":"Synthesis of sulfonylthioureas as anti-diabetic drugs","abstract":"This dissertation discussed the synthesis, cytotoxicity and alpha-glucosidase inhibition of sulfonamides and novel sulfonylthiourea compounds. Three series of novel sulfonylthiourea [benzamido-benzenesulfonylthiourea (28a-28d), pyrrolidino-benzenesulfonylthiourea (33a-33c) and acetamido-benzenesulfonylthiourea (26a-26k) were successfully synthesized in moderate yields to excellent yields. Four novel benzamido-benzenesulfonylthiourea 28a, 28b, 28c and 28d were obtained from reactions of benzamido-benzenesulfonamide with four isothiocyanates. Three novel pyrrolidino benzenesulfonylthiourea 33a, 33b and 33c were obtained from the reactions of pyrrolidino benzenesulfonamide with three isothiocyanates. Five acetamido-benzenesulfonylthioureas 26a-26k were obtained from reactions of acetamido-benzenesulfonamide with four different isothiocyanates. All synthesized compounds were successfully characterized by 1H NMR, 13C NMR, DEPT 135, mass spectrometry and melting points. Benzenesulfonamides 25a-25e, 32, and 27, benzenesulfonylthioureas 28a-28d, 33c, 26a-26e were subjected to in-vitro cyctotoxicity screening against Caco2 cells at concentration of 100 μM and were found to be non-toxic against Caco2 cells. These compounds were then subjected to in-vitro α-glucosidase inhibition study at concentrations of 10 μM, 50 μM, 100 μM and 200 μM. 4-(2-Morpholine-acetamido)-benzenesulfonamide 25-e showed the most promising α-glucosidase inhibition with 95% inhibition at concentration of 50 μM and 98 % inhibition at concentration of 100 μM. Compounds 28-c, 26-b, 26-c and 26-d showed significant improved α-glucosidase inhibition at 200 μM concentration with percent inhibition ranging between 50% and 81%. The study revealed that both sulfonamides and sulfonylthiourea can potentially be used as anti-diabetic agents.","abstract_html":"This dissertation discussed the synthesis, cytotoxicity and alpha-glucosidase inhibition of sulfonamides and novel sulfonylthiourea compounds. Three series of novel sulfonylthiourea [benzamido-benzenesulfonylthiourea (28a-28d), pyrrolidino-benzenesulfonylthiourea (33a-33c) and acetamido-benzenesulfonylthiourea (26a-26k) were successfully synthesized in moderate yields to excellent yields. Four novel benzamido-benzenesulfonylthiourea 28a, 28b, 28c and 28d were obtained from reactions of benzamido-benzenesulfonamide with four isothiocyanates. Three novel pyrrolidino benzenesulfonylthiourea 33a, 33b and 33c were obtained from the reactions of pyrrolidino benzenesulfonamide with three isothiocyanates. Five acetamido-benzenesulfonylthioureas 26a-26k were obtained from reactions of acetamido-benzenesulfonamide with four different isothiocyanates. All synthesized compounds were successfully characterized by 1H NMR, 13C NMR, DEPT 135, mass spectrometry and melting points. Benzenesulfonamides 25a-25e, 32, and 27, benzenesulfonylthioureas 28a-28d, 33c, 26a-26e were subjected to in-vitro cyctotoxicity screening against Caco2 cells at concentration of 100 μM and were found to be non-toxic against Caco2 cells. These compounds were then subjected to in-vitro α-glucosidase inhibition study at concentrations of 10 μM, 50 μM, 100 μM and 200 μM. 4-(2-Morpholine-acetamido)-benzenesulfonamide 25-e showed the most promising α-glucosidase inhibition with 95% inhibition at concentration of 50 μM and 98 % inhibition at concentration of 100 μM. Compounds 28-c, 26-b, 26-c and 26-d showed significant improved α-glucosidase inhibition at 200 μM concentration with percent inhibition ranging between 50% and 81%. The study revealed that both sulfonamides and sulfonylthiourea can potentially be used as anti-diabetic agents.","abstract_has_math":false,"creators":["Tshifaro, Bongani Steven"],"institution":null,"degree_name":null,"degree_level":null,"degree_discipline":null,"degree_department":null,"school":null,"contributors":[],"advisors":[],"committee_chairs":[],"committee_members":[],"year":2026,"date_issued":"2026-05-19","date_published":"2026-05-19","updated_at":"2026-07-27T21:57:59Z","subjects":["Anti-diabetes","In-vitro cytotoxicity","In-vitro a-glucosidase inhibition","Sulfonamides","Sulfonylthioreas","UCTD"],"languages":["en"],"rights":[],"rights_urls":[],"identifier_entries":[]},"links":{"outbound_url":"https://univendspace.univen.ac.za/handle/11602/3190","outbound_label":"Repository record","outbound_source":"dc:identifier.uri"},"metadata_groups":[{"id":"people","label":"People","entries":[{"key":"dc:creator","label":"Author","values":["Tshifaro, Bongani Steven"]}]},{"id":"academic_context","label":"Academic Context","entries":[{"key":"dc:date.accessioned","label":"Dc Date Accessioned","values":["2026-06-17T14:12:21Z"]},{"key":"dc:date.available","label":"Dc Date Available","values":["2026-06-17T14:12:21Z"]},{"key":"dc:date.issued","label":"Date","values":["2026-05-19"]},{"key":"dc:type","label":"Dc Type","values":["Dissertation"]}]},{"id":"subjects_keywords","label":"Subjects and Keywords","entries":[{"key":"dc:subject","label":"Dc Subject","values":["Anti-diabetes","In-vitro cytotoxicity","In-vitro a-glucosidase inhibition","Sulfonamides","Sulfonylthioreas","UCTD"]}]},{"id":"language_rights","label":"Language and Rights","entries":[{"key":"dc:language.iso","label":"Language (ISO)","values":["en"]}]},{"id":"identifiers","label":"Identifiers","entries":[{"key":"dc:identifier.uri","label":"Identifier URI","values":["https://univendspace.univen.ac.za/handle/11602/3190"]}]},{"id":"additional","label":"Additional Metadata","entries":[{"key":"dc:description","label":"Description","values":["M.Sc. in Chemistry"]},{"key":"dc:description.abstract","label":"Abstract","values":["This dissertation discussed the synthesis, cytotoxicity and alpha-glucosidase inhibition of sulfonamides and novel sulfonylthiourea compounds. Three series of novel sulfonylthiourea [benzamido-benzenesulfonylthiourea (28a-28d), pyrrolidino-benzenesulfonylthiourea (33a-33c) and acetamido-benzenesulfonylthiourea (26a-26k) were successfully synthesized in moderate yields to excellent yields. Four novel benzamido-benzenesulfonylthiourea 28a, 28b, 28c and 28d were obtained from reactions of benzamido-benzenesulfonamide with four isothiocyanates. Three novel pyrrolidino benzenesulfonylthiourea 33a, 33b and 33c were obtained from the reactions of pyrrolidino benzenesulfonamide with three isothiocyanates. Five acetamido-benzenesulfonylthioureas 26a-26k were obtained from reactions of acetamido-benzenesulfonamide with four different isothiocyanates. All synthesized compounds were successfully characterized by 1H NMR, 13C NMR, DEPT 135, mass spectrometry and melting points. Benzenesulfonamides 25a-25e, 32, and 27, benzenesulfonylthioureas 28a-28d, 33c, 26a-26e were subjected to in-vitro cyctotoxicity screening against Caco2 cells at concentration of 100 μM and were found to be non-toxic against Caco2 cells. These compounds were then subjected to in-vitro α-glucosidase inhibition study at concentrations of 10 μM, 50 μM, 100 μM and 200 μM. 4-(2-Morpholine-acetamido)-benzenesulfonamide 25-e showed the most promising α-glucosidase inhibition with 95% inhibition at concentration of 50 μM and 98 % inhibition at concentration of 100 μM. Compounds 28-c, 26-b, 26-c and 26-d showed significant improved α-glucosidase inhibition at 200 μM concentration with percent inhibition ranging between 50% and 81%. The study revealed that both sulfonamides and sulfonylthiourea can potentially be used as anti-diabetic agents."]},{"key":"dc:title","label":"Title","values":["Synthesis of sulfonylthioureas as anti-diabetic drugs"]}]}],"canonical_facts":{"dc:creator":["Tshifaro, Bongani Steven"],"dc:date.accessioned":["2026-06-17T14:12:21Z"],"dc:date.available":["2026-06-17T14:12:21Z"],"dc:date.issued":["2026-05-19"],"dc:description":["M.Sc. in Chemistry"],"dc:description.abstract":["This dissertation discussed the synthesis, cytotoxicity and alpha-glucosidase inhibition of sulfonamides and novel sulfonylthiourea compounds. Three series of novel sulfonylthiourea [benzamido-benzenesulfonylthiourea (28a-28d), pyrrolidino-benzenesulfonylthiourea (33a-33c) and acetamido-benzenesulfonylthiourea (26a-26k) were successfully synthesized in moderate yields to excellent yields. Four novel benzamido-benzenesulfonylthiourea 28a, 28b, 28c and 28d were obtained from reactions of benzamido-benzenesulfonamide with four isothiocyanates. Three novel pyrrolidino benzenesulfonylthiourea 33a, 33b and 33c were obtained from the reactions of pyrrolidino benzenesulfonamide with three isothiocyanates. Five acetamido-benzenesulfonylthioureas 26a-26k were obtained from reactions of acetamido-benzenesulfonamide with four different isothiocyanates. All synthesized compounds were successfully characterized by 1H NMR, 13C NMR, DEPT 135, mass spectrometry and melting points. Benzenesulfonamides 25a-25e, 32, and 27, benzenesulfonylthioureas 28a-28d, 33c, 26a-26e were subjected to in-vitro cyctotoxicity screening against Caco2 cells at concentration of 100 μM and were found to be non-toxic against Caco2 cells. These compounds were then subjected to in-vitro α-glucosidase inhibition study at concentrations of 10 μM, 50 μM, 100 μM and 200 μM. 4-(2-Morpholine-acetamido)-benzenesulfonamide 25-e showed the most promising α-glucosidase inhibition with 95% inhibition at concentration of 50 μM and 98 % inhibition at concentration of 100 μM. Compounds 28-c, 26-b, 26-c and 26-d showed significant improved α-glucosidase inhibition at 200 μM concentration with percent inhibition ranging between 50% and 81%. The study revealed that both sulfonamides and sulfonylthiourea can potentially be used as anti-diabetic agents."],"dc:identifier.uri":["https://univendspace.univen.ac.za/handle/11602/3190"],"dc:language.iso":["en"],"dc:subject":["Anti-diabetes","In-vitro cytotoxicity","In-vitro a-glucosidase inhibition","Sulfonamides","Sulfonylthioreas","UCTD"],"dc:title":["Synthesis of sulfonylthioureas as anti-diabetic drugs"],"dc:type":["Dissertation"]},"updated_at":"2026-07-27T21:57:59Z"}