Evaluation and molecular modelling of bis-Schiff base derivatives as potential leads for management of diabetes mellitus
Developing a medication to cure and manage diabetes mellitus complications is of interest in medicinal chemistry. Toward this end, six bis-biphenyl-salicylaldehyde Schiff base derivatives have been evaluated for their α-glucosidase inhibition, antiglycation and anti-inflammation potentials. Four com...
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| Format: | Article |
| Language: | English |
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Sciendo
2022-09-01
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| Series: | Acta Pharmaceutica |
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| Online Access: | https://doi.org/10.2478/acph-2022-0019 |
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| author | Daoud Safa Thiab Samar Jazzazi Taghreed M. A. Al-Shboul Tareq M. A. Ullah Saeed |
| author_facet | Daoud Safa Thiab Samar Jazzazi Taghreed M. A. Al-Shboul Tareq M. A. Ullah Saeed |
| author_sort | Daoud Safa |
| collection | DOAJ |
| description | Developing a medication to cure and manage diabetes mellitus complications is of interest in medicinal chemistry. Toward this end, six bis-biphenyl-salicylaldehyde Schiff base derivatives have been evaluated for their α-glucosidase inhibition, antiglycation and anti-inflammation potentials. Four compounds (compounds 2–5) showed an excellent α-glucosidase inhibitory effect superior to that produced by acarbose. Additionally, the docking study revealed that these compounds are anchored within the binding pocket of α-glucosidase via hydrogen bonding, π-stacking and hydrophobic interactions, comparable to a high number of hydrogen bonding involved in anchoring acarbose. Interestingly, all tested compounds showed varying degrees of antiglycation activity with superior activity for two of them (compound 1 and compound 6) compared to the standard rutin. Moreover, the results indicated an outstanding anti-inflammatory activity for two compounds (compounds 1 and 6) compared to ibuprofen. |
| format | Article |
| id | doaj-art-eac0f7e8c6a94c6d86eb43b88fbaa3f6 |
| institution | Kabale University |
| issn | 1846-9558 |
| language | English |
| publishDate | 2022-09-01 |
| publisher | Sciendo |
| record_format | Article |
| series | Acta Pharmaceutica |
| spelling | doaj-art-eac0f7e8c6a94c6d86eb43b88fbaa3f62025-02-02T05:15:57ZengSciendoActa Pharmaceutica1846-95582022-09-0172344945810.2478/acph-2022-0019Evaluation and molecular modelling of bis-Schiff base derivatives as potential leads for management of diabetes mellitusDaoud Safa0Thiab Samar1Jazzazi Taghreed M. A.2Al-Shboul Tareq M. A.3Ullah Saeed4Department of Pharmaceutical Chemistry and Pharmacognosy Faculty of Pharmacy, Applied Science Private University, Amman, JordanDepartment of Pharmaceutical Chemistry and Pharmacognosy Faculty of Pharmacy, Applied Science Private University, Amman, JordanDepartment of Chemistry, Yarmouk University, Irbid, JordanDepartment of Chemistry and Chemical Technology, Tafila Technical University Tafila, JordanH. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences University of Karachi, Karachi-75270PakistanDeveloping a medication to cure and manage diabetes mellitus complications is of interest in medicinal chemistry. Toward this end, six bis-biphenyl-salicylaldehyde Schiff base derivatives have been evaluated for their α-glucosidase inhibition, antiglycation and anti-inflammation potentials. Four compounds (compounds 2–5) showed an excellent α-glucosidase inhibitory effect superior to that produced by acarbose. Additionally, the docking study revealed that these compounds are anchored within the binding pocket of α-glucosidase via hydrogen bonding, π-stacking and hydrophobic interactions, comparable to a high number of hydrogen bonding involved in anchoring acarbose. Interestingly, all tested compounds showed varying degrees of antiglycation activity with superior activity for two of them (compound 1 and compound 6) compared to the standard rutin. Moreover, the results indicated an outstanding anti-inflammatory activity for two compounds (compounds 1 and 6) compared to ibuprofen.https://doi.org/10.2478/acph-2022-0019bis-schiff basesdiabetes mellitusglycationpostprandial hyperglycemiaα-glucosidasedocking study |
| spellingShingle | Daoud Safa Thiab Samar Jazzazi Taghreed M. A. Al-Shboul Tareq M. A. Ullah Saeed Evaluation and molecular modelling of bis-Schiff base derivatives as potential leads for management of diabetes mellitus Acta Pharmaceutica bis-schiff bases diabetes mellitus glycation postprandial hyperglycemia α-glucosidase docking study |
| title | Evaluation and molecular modelling of bis-Schiff base derivatives as potential leads for management of diabetes mellitus |
| title_full | Evaluation and molecular modelling of bis-Schiff base derivatives as potential leads for management of diabetes mellitus |
| title_fullStr | Evaluation and molecular modelling of bis-Schiff base derivatives as potential leads for management of diabetes mellitus |
| title_full_unstemmed | Evaluation and molecular modelling of bis-Schiff base derivatives as potential leads for management of diabetes mellitus |
| title_short | Evaluation and molecular modelling of bis-Schiff base derivatives as potential leads for management of diabetes mellitus |
| title_sort | evaluation and molecular modelling of bis schiff base derivatives as potential leads for management of diabetes mellitus |
| topic | bis-schiff bases diabetes mellitus glycation postprandial hyperglycemia α-glucosidase docking study |
| url | https://doi.org/10.2478/acph-2022-0019 |
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