Synthesis, Characterisation And Molecular Docking Of Quinoxaline-isoxazole Hybrids As Potential Anti-hyperglycemic Agent
Diabetes mellitus is a chronic metabolic disorder that affects millions of people worldwide, leading to severe complications such as cardiovascular disease, obesity, and retinopathy. Despite advances in treatment, effective management of diabetes remains a significant challenge due to the limitation...
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| Format: | Thesis |
| Language: | English |
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2024
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| Online Access: | http://eprints.usm.my/62064/ http://eprints.usm.my/62064/1/LACKSANY%20PHONGPHANE%20-%20TESIS24.pdf |
| _version_ | 1848884879877472256 |
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| author | Phongphane, Lacksany |
| author_facet | Phongphane, Lacksany |
| author_sort | Phongphane, Lacksany |
| building | USM Institutional Repository |
| collection | Online Access |
| description | Diabetes mellitus is a chronic metabolic disorder that affects millions of people worldwide, leading to severe complications such as cardiovascular disease, obesity, and retinopathy. Despite advances in treatment, effective management of diabetes remains a significant challenge due to the limitations of current therapeutic options, including side effects and limited efficacy in controlling blood glucose levels. Hence, in our effort to develop anti-hyperglycemic agents that potentially inhibiting α-amylase and α-glucosidase enzymes, a series of new quinoxaline-isoxazole hybrids were successfully synthesised via five-step cyclisation. The new quinoxaline-isoxazole derivatives (84a-84v) were successful synthesised and obtained twenty-two compounds in a good yield within the range of 54% to 95%. Subsequently, these synthesised compounds were characterised and elucidated by several spectroscopies methods consisting of Fourier transform-infrared (FT-IR), and nuclear magnetic resonance (1D and 2D-NMR) including high-resolution mass spectrometry (HRMS). The synthesised compounds were further evaluated for the in vitro -amylase and -glucosidase inhibitory activities using acarbose as a positive control. Among 22 synthesised compounds, the results revealed that compound 84j showed dual inhibitory towards -amylase and -glucosidase with promising IC50 values of 17.0 and 40.1 μM, respectively. Moreover, compound 84c was also displayed the good dual activity for the inhibition of -amylase (IC50 = 24.0 μM) and -glucosidase (IC50 = 41.7 μM). |
| first_indexed | 2025-11-15T19:13:43Z |
| format | Thesis |
| id | usm-62064 |
| institution | Universiti Sains Malaysia |
| institution_category | Local University |
| language | English |
| last_indexed | 2025-11-15T19:13:43Z |
| publishDate | 2024 |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | usm-620642025-03-26T01:51:57Z http://eprints.usm.my/62064/ Synthesis, Characterisation And Molecular Docking Of Quinoxaline-isoxazole Hybrids As Potential Anti-hyperglycemic Agent Phongphane, Lacksany QD1-65 General Including alchemy Diabetes mellitus is a chronic metabolic disorder that affects millions of people worldwide, leading to severe complications such as cardiovascular disease, obesity, and retinopathy. Despite advances in treatment, effective management of diabetes remains a significant challenge due to the limitations of current therapeutic options, including side effects and limited efficacy in controlling blood glucose levels. Hence, in our effort to develop anti-hyperglycemic agents that potentially inhibiting α-amylase and α-glucosidase enzymes, a series of new quinoxaline-isoxazole hybrids were successfully synthesised via five-step cyclisation. The new quinoxaline-isoxazole derivatives (84a-84v) were successful synthesised and obtained twenty-two compounds in a good yield within the range of 54% to 95%. Subsequently, these synthesised compounds were characterised and elucidated by several spectroscopies methods consisting of Fourier transform-infrared (FT-IR), and nuclear magnetic resonance (1D and 2D-NMR) including high-resolution mass spectrometry (HRMS). The synthesised compounds were further evaluated for the in vitro -amylase and -glucosidase inhibitory activities using acarbose as a positive control. Among 22 synthesised compounds, the results revealed that compound 84j showed dual inhibitory towards -amylase and -glucosidase with promising IC50 values of 17.0 and 40.1 μM, respectively. Moreover, compound 84c was also displayed the good dual activity for the inhibition of -amylase (IC50 = 24.0 μM) and -glucosidase (IC50 = 41.7 μM). 2024-09 Thesis NonPeerReviewed application/pdf en http://eprints.usm.my/62064/1/LACKSANY%20PHONGPHANE%20-%20TESIS24.pdf Phongphane, Lacksany (2024) Synthesis, Characterisation And Molecular Docking Of Quinoxaline-isoxazole Hybrids As Potential Anti-hyperglycemic Agent. PhD thesis, Universiti Sains Malaysia. |
| spellingShingle | QD1-65 General Including alchemy Phongphane, Lacksany Synthesis, Characterisation And Molecular Docking Of Quinoxaline-isoxazole Hybrids As Potential Anti-hyperglycemic Agent |
| title | Synthesis, Characterisation And Molecular Docking Of Quinoxaline-isoxazole Hybrids As Potential Anti-hyperglycemic Agent |
| title_full | Synthesis, Characterisation And Molecular Docking Of Quinoxaline-isoxazole Hybrids As Potential Anti-hyperglycemic Agent |
| title_fullStr | Synthesis, Characterisation And Molecular Docking Of Quinoxaline-isoxazole Hybrids As Potential Anti-hyperglycemic Agent |
| title_full_unstemmed | Synthesis, Characterisation And Molecular Docking Of Quinoxaline-isoxazole Hybrids As Potential Anti-hyperglycemic Agent |
| title_short | Synthesis, Characterisation And Molecular Docking Of Quinoxaline-isoxazole Hybrids As Potential Anti-hyperglycemic Agent |
| title_sort | synthesis, characterisation and molecular docking of quinoxaline-isoxazole hybrids as potential anti-hyperglycemic agent |
| topic | QD1-65 General Including alchemy |
| url | http://eprints.usm.my/62064/ http://eprints.usm.my/62064/1/LACKSANY%20PHONGPHANE%20-%20TESIS24.pdf |