Investigating Novel Thiophene Carbaldehyde Based Thiazole Derivatives as Potential Hits for Diabetic Management: Synthesis, In Vitro and In Silico Approach
This research work is based on synthesis of eleven novel thiazole derivatives (3 a-k) of thiophene carbaldehyde. All the synthesized compounds were successfully synthesized, characterized by 1H-NMR and EI-MS spectroscopic techniques and finally subjected for their in vitro α-glucosidase inhibitory a...
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John Wiley and Sons Inc
2024
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| Online Access: | https://www.scopus.com/inward/record.uri?eid=2-s2.0-85185670155&doi=10.1002%2fslct.202304601&partnerID=40&md5=40b953aa5768f9105d5cf00e558df6ec |
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2-s2.0-85185670155 Ullah N.; Alam A.; Zainab; Elhenawy A.A.; Naz S.; Islam M.S.; Ahmad S.; Shah S.A.A.; Ahmad M. Investigating Novel Thiophene Carbaldehyde Based Thiazole Derivatives as Potential Hits for Diabetic Management: Synthesis, In Vitro and In Silico Approach 2024 ChemistrySelect 9 8 10.1002/slct.202304601 https://www.scopus.com/inward/record.uri?eid=2-s2.0-85185670155&doi=10.1002%2fslct.202304601&partnerID=40&md5=40b953aa5768f9105d5cf00e558df6ec This research work is based on synthesis of eleven novel thiazole derivatives (3 a-k) of thiophene carbaldehyde. All the synthesized compounds were successfully synthesized, characterized by 1H-NMR and EI-MS spectroscopic techniques and finally subjected for their in vitro α-glucosidase inhibitory activity. Seven derivatives 3 i (IC50=10.21±1.84 μM), 3 b (IC50=11.14±0.99 μM), 3 f (IC50=13.21±2.76 μM), 3 h (IC50=14.21±0.31 μM), 3 k (IC50=15.21±1.02 μM), 3 e (IC50=16.21±1.32 μM), and 3 c (IC50=18.21±1.89 μM), in the series displayed excellent inhibitory potential better than the standard acarbose. However, two compounds 3 g (IC50=33.21±1.99 μM) and 3 d (IC50=42.31±2.12 μM) showed significant activity while two compounds 3 j and 3 a were found less active with IC50 values of 82.31±0.31 and 88.36±1.21 μM respectively. Additional research revealed that the compounds are not exhibiting any cytotoxic effects. The molecular docking study of these derivatives showed their good binding potential for α-glucosidase active site with excellent interactions and docking scores. © 2024 Wiley-VCH GmbH. John Wiley and Sons Inc 23656549 English Article |
| author |
Ullah N.; Alam A.; Zainab; Elhenawy A.A.; Naz S.; Islam M.S.; Ahmad S.; Shah S.A.A.; Ahmad M. |
| spellingShingle |
Ullah N.; Alam A.; Zainab; Elhenawy A.A.; Naz S.; Islam M.S.; Ahmad S.; Shah S.A.A.; Ahmad M. Investigating Novel Thiophene Carbaldehyde Based Thiazole Derivatives as Potential Hits for Diabetic Management: Synthesis, In Vitro and In Silico Approach |
| author_facet |
Ullah N.; Alam A.; Zainab; Elhenawy A.A.; Naz S.; Islam M.S.; Ahmad S.; Shah S.A.A.; Ahmad M. |
| author_sort |
Ullah N.; Alam A.; Zainab; Elhenawy A.A.; Naz S.; Islam M.S.; Ahmad S.; Shah S.A.A.; Ahmad M. |
| title |
Investigating Novel Thiophene Carbaldehyde Based Thiazole Derivatives as Potential Hits for Diabetic Management: Synthesis, In Vitro and In Silico Approach |
| title_short |
Investigating Novel Thiophene Carbaldehyde Based Thiazole Derivatives as Potential Hits for Diabetic Management: Synthesis, In Vitro and In Silico Approach |
| title_full |
Investigating Novel Thiophene Carbaldehyde Based Thiazole Derivatives as Potential Hits for Diabetic Management: Synthesis, In Vitro and In Silico Approach |
| title_fullStr |
Investigating Novel Thiophene Carbaldehyde Based Thiazole Derivatives as Potential Hits for Diabetic Management: Synthesis, In Vitro and In Silico Approach |
| title_full_unstemmed |
Investigating Novel Thiophene Carbaldehyde Based Thiazole Derivatives as Potential Hits for Diabetic Management: Synthesis, In Vitro and In Silico Approach |
| title_sort |
Investigating Novel Thiophene Carbaldehyde Based Thiazole Derivatives as Potential Hits for Diabetic Management: Synthesis, In Vitro and In Silico Approach |
| publishDate |
2024 |
| container_title |
ChemistrySelect |
| container_volume |
9 |
| container_issue |
8 |
| doi_str_mv |
10.1002/slct.202304601 |
| url |
https://www.scopus.com/inward/record.uri?eid=2-s2.0-85185670155&doi=10.1002%2fslct.202304601&partnerID=40&md5=40b953aa5768f9105d5cf00e558df6ec |
| description |
This research work is based on synthesis of eleven novel thiazole derivatives (3 a-k) of thiophene carbaldehyde. All the synthesized compounds were successfully synthesized, characterized by 1H-NMR and EI-MS spectroscopic techniques and finally subjected for their in vitro α-glucosidase inhibitory activity. Seven derivatives 3 i (IC50=10.21±1.84 μM), 3 b (IC50=11.14±0.99 μM), 3 f (IC50=13.21±2.76 μM), 3 h (IC50=14.21±0.31 μM), 3 k (IC50=15.21±1.02 μM), 3 e (IC50=16.21±1.32 μM), and 3 c (IC50=18.21±1.89 μM), in the series displayed excellent inhibitory potential better than the standard acarbose. However, two compounds 3 g (IC50=33.21±1.99 μM) and 3 d (IC50=42.31±2.12 μM) showed significant activity while two compounds 3 j and 3 a were found less active with IC50 values of 82.31±0.31 and 88.36±1.21 μM respectively. Additional research revealed that the compounds are not exhibiting any cytotoxic effects. The molecular docking study of these derivatives showed their good binding potential for α-glucosidase active site with excellent interactions and docking scores. © 2024 Wiley-VCH GmbH. |
| publisher |
John Wiley and Sons Inc |
| issn |
23656549 |
| language |
English |
| format |
Article |
| accesstype |
|
| record_format |
scopus |
| collection |
Scopus |
| _version_ |
1814778499986096128 |