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- Publisher Website: 10.1038/s41598-017-05895-9
- Scopus: eid_2-s2.0-85025126555
- PMID: 28717146
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Article: Concise and Stereodivergent Synthesis of Carbasugars Reveals Unexpected Structure-Activity Relationship (SAR) of SGLT2 Inhibition
Title | Concise and Stereodivergent Synthesis of Carbasugars Reveals Unexpected Structure-Activity Relationship (SAR) of SGLT2 Inhibition |
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Authors | |
Issue Date | 2017 |
Citation | Scientific Reports, 2017, v. 7, n. 1, article no. 5581 How to Cite? |
Abstract | Carbasugar sodium-glucose cotransporter 2 (SGLT2) inhibitors are highly promising drug candidates for the treatment of Type 2 diabetes mellitus (T2DM). However, the clinical usage of carbasugar SGLT2 inhibitors has been underexplored, due to the lengthy synthetic routes and the lack of structure-activity relationship (SAR) studies of these compounds. Herein, we report a concise and stereodivergent synthetic route towards some novel carbasugar SGLT2 inhibitors, featuring an underexploited, regioselective, and stereospecific palladium-catalyzed allyl-aryl coupling reaction. This synthetic strategy, together with computational modeling, revealed the unexpected SAR of these carbasugar SGLT2 inhibitors, and enabled the discovery of a highly selective and potent SGLT2 inhibitor. |
Persistent Identifier | http://hdl.handle.net/10722/343243 |
DC Field | Value | Language |
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dc.contributor.author | Ng, Wai Lung | - |
dc.contributor.author | Li, Ho Chuen | - |
dc.contributor.author | Lau, Kit Man | - |
dc.contributor.author | Chan, Anthony K.N. | - |
dc.contributor.author | Lau, Clara Bik San | - |
dc.contributor.author | Shing, Tony K.M. | - |
dc.date.accessioned | 2024-05-10T09:06:34Z | - |
dc.date.available | 2024-05-10T09:06:34Z | - |
dc.date.issued | 2017 | - |
dc.identifier.citation | Scientific Reports, 2017, v. 7, n. 1, article no. 5581 | - |
dc.identifier.uri | http://hdl.handle.net/10722/343243 | - |
dc.description.abstract | Carbasugar sodium-glucose cotransporter 2 (SGLT2) inhibitors are highly promising drug candidates for the treatment of Type 2 diabetes mellitus (T2DM). However, the clinical usage of carbasugar SGLT2 inhibitors has been underexplored, due to the lengthy synthetic routes and the lack of structure-activity relationship (SAR) studies of these compounds. Herein, we report a concise and stereodivergent synthetic route towards some novel carbasugar SGLT2 inhibitors, featuring an underexploited, regioselective, and stereospecific palladium-catalyzed allyl-aryl coupling reaction. This synthetic strategy, together with computational modeling, revealed the unexpected SAR of these carbasugar SGLT2 inhibitors, and enabled the discovery of a highly selective and potent SGLT2 inhibitor. | - |
dc.language | eng | - |
dc.relation.ispartof | Scientific Reports | - |
dc.title | Concise and Stereodivergent Synthesis of Carbasugars Reveals Unexpected Structure-Activity Relationship (SAR) of SGLT2 Inhibition | - |
dc.type | Article | - |
dc.description.nature | link_to_subscribed_fulltext | - |
dc.identifier.doi | 10.1038/s41598-017-05895-9 | - |
dc.identifier.pmid | 28717146 | - |
dc.identifier.scopus | eid_2-s2.0-85025126555 | - |
dc.identifier.volume | 7 | - |
dc.identifier.issue | 1 | - |
dc.identifier.spage | article no. 5581 | - |
dc.identifier.epage | article no. 5581 | - |
dc.identifier.eissn | 2045-2322 | - |