Synthesis, in-vivo anti-diabetic & anticancer activities and molecular modelling studies of tetrahydro benzo[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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Format: | Article |
Language: | English English |
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King Saud University
2021
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Online Access: | https://eprints.ums.edu.my/id/eprint/33239/1/Synthesis%2C%20in-vivo%20anti-diabetic%20%26%20anticancer%20activities%20and%20molecular%20modelling%20studies%20of%20tetrahydro%20benzo%5Bd%5Dthiazole%20tethered%20nicotinohydrazide%20derivatives.pdf https://eprints.ums.edu.my/id/eprint/33239/2/Synthesis%2C%20in-vivo%20anti-diabetic%20%26%20anticancer%20activities%20and%20molecular%20modelling%20studies%20of%20tetrahydro%20benzo%5Bd%5Dthiazole%20tethered%20nicotinohydrazide%20derivatives1.pdf https://eprints.ums.edu.my/id/eprint/33239/ https://www.sciencedirect.com/science/article/pii/S187853522100561X https://doi.org/10.1016/j.arabjc.2021.103546 |
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Summary: | 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-c 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. |
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