Synthesis, in-vivo anti-diabetic & anticancer activities and molecular modelling studies of tetrahydrobenzo[d]thiazole tethered nicotinohydrazide derivatives
A series of thirty new thiazole-pyridine derivatives were synthesized by reaction of 4,4,7,7-tetra-methyl-4,5,6,7-tetrahydrobenzo[d]thiazol-2-amine with 6-chloronicotinate followed by condensing with benzaldehydes and screened for their anti-diabetic activity by in vivo housing Swiss albino mice. Al...
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| Формат: | Статья |
| Язык: | English English |
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Elsevier
2022
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| Online-ссылка: | https://eprints.ums.edu.my/id/eprint/28959/2/Synthesis%2C%20in-vivo%20anti-diabetic%20%26%20anticancer%20activities%20and%20molecular%20modelling%20studies%20of%20tetrahydrobenzo%5Bd%5Dthiazole%20tethered%20nicotinohydrazide%20derivatives.pdf https://eprints.ums.edu.my/id/eprint/28959/3/Synthesis%2C%20in-vivo%20anti-diabetic%20%26%20anticancer%20activities%20and%20molecular%20modelling%20studies%20of%20tetrahydrobenzo%5Bd%5Dthiazole%20tethered%20nicotinohydrazide%20derivatives%20_ABSTRACT.pdf |
| _version_ | 1825714204890365952 |
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| author | Suri Babu Patchipala Pasupuleti Visweswara Rao Amrutha V Audipudi Hari babu Bollikolla |
| author_facet | Suri Babu Patchipala Pasupuleti Visweswara Rao Amrutha V Audipudi Hari babu Bollikolla |
| author_sort | Suri Babu Patchipala |
| collection | UMS |
| description | A series of thirty new thiazole-pyridine derivatives were synthesized by reaction of 4,4,7,7-tetra-methyl-4,5,6,7-tetrahydrobenzo[d]thiazol-2-amine with 6-chloronicotinate followed by condensing with benzaldehydes and screened for their anti-diabetic activity by in vivo housing Swiss albino mice. All synthesized compounds resulted in reducing the glucose level when compared with reference standard drug glibenclamide. In specific, compound 7 exhibited significant activity in terms of fasting blood glucose level reduction. In addition, the in-silico binding studies of the potential compounds 11f and 11g with human PPAR-γ protein complexed with Retinoid X Receptor (RXR) alpha Nuclear Receptor showed good interactions when compared to the standard drug Rosiglitazone. The newly synthesized drugs may be potential anti-diabetic drugs with possible specific actions. |
| first_indexed | 2024-03-06T03:08:20Z |
| format | Article |
| id | ums.eprints-28959 |
| institution | Universiti Malaysia Sabah |
| language | English English |
| last_indexed | 2024-03-06T03:08:20Z |
| publishDate | 2022 |
| publisher | Elsevier |
| record_format | dspace |
| spelling | ums.eprints-289592022-07-28T00:19:49Z https://eprints.ums.edu.my/id/eprint/28959/ Synthesis, in-vivo anti-diabetic & anticancer activities and molecular modelling studies of tetrahydrobenzo[d]thiazole tethered nicotinohydrazide derivatives Suri Babu Patchipala Pasupuleti Visweswara Rao Amrutha V Audipudi Hari babu Bollikolla RC31-1245 Internal medicine A series of thirty new thiazole-pyridine derivatives were synthesized by reaction of 4,4,7,7-tetra-methyl-4,5,6,7-tetrahydrobenzo[d]thiazol-2-amine with 6-chloronicotinate followed by condensing with benzaldehydes and screened for their anti-diabetic activity by in vivo housing Swiss albino mice. All synthesized compounds resulted in reducing the glucose level when compared with reference standard drug glibenclamide. In specific, compound 7 exhibited significant activity in terms of fasting blood glucose level reduction. In addition, the in-silico binding studies of the potential compounds 11f and 11g with human PPAR-γ protein complexed with Retinoid X Receptor (RXR) alpha Nuclear Receptor showed good interactions when compared to the standard drug Rosiglitazone. The newly synthesized drugs may be potential anti-diabetic drugs with possible specific actions. Elsevier 2022 Article PeerReviewed text en https://eprints.ums.edu.my/id/eprint/28959/2/Synthesis%2C%20in-vivo%20anti-diabetic%20%26%20anticancer%20activities%20and%20molecular%20modelling%20studies%20of%20tetrahydrobenzo%5Bd%5Dthiazole%20tethered%20nicotinohydrazide%20derivatives.pdf text en https://eprints.ums.edu.my/id/eprint/28959/3/Synthesis%2C%20in-vivo%20anti-diabetic%20%26%20anticancer%20activities%20and%20molecular%20modelling%20studies%20of%20tetrahydrobenzo%5Bd%5Dthiazole%20tethered%20nicotinohydrazide%20derivatives%20_ABSTRACT.pdf Suri Babu Patchipala and Pasupuleti Visweswara Rao and Amrutha V Audipudi and Hari babu Bollikolla (2022) Synthesis, in-vivo anti-diabetic & anticancer activities and molecular modelling studies of tetrahydrobenzo[d]thiazole tethered nicotinohydrazide derivatives. Arabian Journal of Chemistry, 15 (103546). pp. 1-12. ISSN 1878-5352 https://www.sciencedirect.com/science/article/pii/S187853522100561X https://doi.org/10.1016/j.arabjc.2021.103546 https://doi.org/10.1016/j.arabjc.2021.103546 |
| spellingShingle | RC31-1245 Internal medicine Suri Babu Patchipala Pasupuleti Visweswara Rao Amrutha V Audipudi Hari babu Bollikolla Synthesis, in-vivo anti-diabetic & anticancer activities and molecular modelling studies of tetrahydrobenzo[d]thiazole tethered nicotinohydrazide derivatives |
| title | Synthesis, in-vivo anti-diabetic & anticancer activities and molecular modelling studies of tetrahydrobenzo[d]thiazole tethered nicotinohydrazide derivatives |
| title_full | Synthesis, in-vivo anti-diabetic & anticancer activities and molecular modelling studies of tetrahydrobenzo[d]thiazole tethered nicotinohydrazide derivatives |
| title_fullStr | Synthesis, in-vivo anti-diabetic & anticancer activities and molecular modelling studies of tetrahydrobenzo[d]thiazole tethered nicotinohydrazide derivatives |
| title_full_unstemmed | Synthesis, in-vivo anti-diabetic & anticancer activities and molecular modelling studies of tetrahydrobenzo[d]thiazole tethered nicotinohydrazide derivatives |
| title_short | Synthesis, in-vivo anti-diabetic & anticancer activities and molecular modelling studies of tetrahydrobenzo[d]thiazole tethered nicotinohydrazide derivatives |
| title_sort | synthesis in vivo anti diabetic anticancer activities and molecular modelling studies of tetrahydrobenzo d thiazole tethered nicotinohydrazide derivatives |
| topic | RC31-1245 Internal medicine |
| url | https://eprints.ums.edu.my/id/eprint/28959/2/Synthesis%2C%20in-vivo%20anti-diabetic%20%26%20anticancer%20activities%20and%20molecular%20modelling%20studies%20of%20tetrahydrobenzo%5Bd%5Dthiazole%20tethered%20nicotinohydrazide%20derivatives.pdf https://eprints.ums.edu.my/id/eprint/28959/3/Synthesis%2C%20in-vivo%20anti-diabetic%20%26%20anticancer%20activities%20and%20molecular%20modelling%20studies%20of%20tetrahydrobenzo%5Bd%5Dthiazole%20tethered%20nicotinohydrazide%20derivatives%20_ABSTRACT.pdf |
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