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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Autores principales: Suri Babu Patchipala, Visweswara Rao Pasupuleti, Amrutha V Audipudi, Hari babu Bollikolla
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Lenguaje:EN
Publicado: Elsevier 2022
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Acceso en línea:https://doaj.org/article/18dfe7a566ba4233b6e4b7b7eb4b529c
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spelling oai:doaj.org-article:18dfe7a566ba4233b6e4b7b7eb4b529c2021-11-28T04:29:34ZSynthesis, in-vivo anti-diabetic & anticancer activities and molecular modelling studies of tetrahydrobenzo[d]thiazole tethered nicotinohydrazide derivatives1878-535210.1016/j.arabjc.2021.103546https://doaj.org/article/18dfe7a566ba4233b6e4b7b7eb4b529c2022-02-01T00:00:00Zhttp://www.sciencedirect.com/science/article/pii/S187853522100561Xhttps://doaj.org/toc/1878-5352A 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.Suri Babu PatchipalaVisweswara Rao PasupuletiAmrutha V AudipudiHari babu BollikollaElsevierarticleTetrahydrothiazolePyridinehydrazideAnti-diabetic activityMolecular modelingChemistryQD1-999ENArabian Journal of Chemistry, Vol 15, Iss 2, Pp 103546- (2022)
institution DOAJ
collection DOAJ
language EN
topic Tetrahydrothiazole
Pyridinehydrazide
Anti-diabetic activity
Molecular modeling
Chemistry
QD1-999
spellingShingle Tetrahydrothiazole
Pyridinehydrazide
Anti-diabetic activity
Molecular modeling
Chemistry
QD1-999
Suri Babu Patchipala
Visweswara Rao Pasupuleti
Amrutha V Audipudi
Hari babu Bollikolla
Synthesis, in-vivo anti-diabetic & anticancer activities and molecular modelling studies of tetrahydrobenzo[d]thiazole tethered nicotinohydrazide derivatives
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.
format article
author Suri Babu Patchipala
Visweswara Rao Pasupuleti
Amrutha V Audipudi
Hari babu Bollikolla
author_facet Suri Babu Patchipala
Visweswara Rao Pasupuleti
Amrutha V Audipudi
Hari babu Bollikolla
author_sort Suri Babu Patchipala
title 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_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_sort synthesis, in-vivo anti-diabetic & anticancer activities and molecular modelling studies of tetrahydrobenzo[d]thiazole tethered nicotinohydrazide derivatives
publisher Elsevier
publishDate 2022
url https://doaj.org/article/18dfe7a566ba4233b6e4b7b7eb4b529c
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AT visweswararaopasupuleti synthesisinvivoantidiabeticampanticanceractivitiesandmolecularmodellingstudiesoftetrahydrobenzodthiazoletetherednicotinohydrazidederivatives
AT amruthavaudipudi synthesisinvivoantidiabeticampanticanceractivitiesandmolecularmodellingstudiesoftetrahydrobenzodthiazoletetherednicotinohydrazidederivatives
AT haribabubollikolla synthesisinvivoantidiabeticampanticanceractivitiesandmolecularmodellingstudiesoftetrahydrobenzodthiazoletetherednicotinohydrazidederivatives
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