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

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

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URL: https://www.sciencedirect.com/science/article/pii/...

Abstract

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.

Item Type:	Article
Keyword:	Tetrahydrothiazole , Pyridinehydrazide , Anti-diabetic activity , Molecular modeling
Subjects:	R Medicine > RC Internal medicine > RC31-1245 Internal medicine
Department:	FACULTY > Faculty of Medicine and Health Sciences
Depositing User:	SAFRUDIN BIN DARUN -
Date Deposited:	28 Jul 2022 08:19
Last Modified:	28 Jul 2022 08:19
URI:	https://eprints.ums.edu.my/id/eprint/28959

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