Synthesis, in-vivo anti-diabetic & anticancer activities and molecular modelling studies of tetrahydro benzo[d]thiazole tethered nicotinohydrazide derivatives

• Main Authors: Suri Babu Patchipala, Visweswara Rao Pasupuleti, Amrutha V Audipudi, Hari babu Bollikolla
• Format: Article
• Language: English; English
• Published: King Saud University 2021
• Subjects: RC254-282 Neoplasms. Tumors. Oncology Including cancer and carcinogens; RC31-1245 Internal medicine
• 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
• Institution: Universiti Malaysia Sabah

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.