Synthesis, Spectral Analysis, <i>In Vitro</i> Microbiological Evaluation, and Molecular Docking Studies of Some Novel 1-(1-Aryl-1<i>H</i>-tetrazol-5-yl)-2-(piperidin-1-yl)ethanone Derivatives

Elavarasan, T.; Bhakiaraj, Durairaj Peter; Gopalakrishnan, Mahesh

doi:10.1155/2014/120173

Cited by 10 publications

(5 citation statements)

References 17 publications

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“…Recently, it has been reported that N -containing heterocycles are considered especially “privileged” structures for the synthesis and development of new drugs. 36,37…”

Section: Resultsmentioning

confidence: 99%

“…Recently, it has been reported that N-containing heterocycles are considered especially ''privileged'' structures for the synthesis and development of new drugs. 36,37 Compounds 7b (bis-benzyloxy substituent), 7f (benzodioxole substituent), and 7g (phenylpyrazole substituent) were the second most active in HepG2, T47D, and Jurkat cell lines, respectively.…”

Section: In Vitro Cytotoxic Activity In Tumor Cellsmentioning

confidence: 99%

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New thiazacridine agents: Synthesis, physical and chemical characterization, and in vitro anticancer evaluation

et al. 2016

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A series of new thiazacridine agents were synthesized and evaluated as antitumor agents, in terms of not only their cytotoxicity but also their selectivity. The cytotoxicity assay confirmed that all compounds showed cytotoxic activity and selectivity. The new compound, 3-acridin-9-ylmethyl-5-(5-bromo-1 H-indol-3-ylmethylene)-thiazolidine-2,4-dione (LPSF/AA29 – 7a), proved to be the most promising compound as it presents lower half-maximal inhibitory concentration (IC50) values (ranging from 0.25 to 68.03 µM) depending on cell lineage. In HepG2 cells, the lowest IC50 value was exhibited by 3-acridin-9-ylmethyl-5-(4-piperidin-1-yl-benzylidene)-thiazolidine-2,4-dione (LPSF/AA36 – 7b; 46.95 µM). None of the synthesized compounds showed cytotoxic activity against normal cells (IC50 > 100 µM). The mechanism of death induction and cell cycle effects was also evaluated. Flow cytometric analysis revealed that the compounds LPSF/AA29 – 7a and LPSF/AA36 – 7b significantly increased the percentage of apoptotic cells and induced G2/M arrest in the cell cycle progression. Therefore, these new thiazacridine derivatives constitute promising antitumor agents whose cytotoxicity and selectivity properties indicate they have potential to contribute to or serve as a basis for the development of new cancer drugs in the future.

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“…Recently, it has been reported that N -containing heterocycles are considered especially “privileged” structures for the synthesis and development of new drugs. 36,37…”

Section: Resultsmentioning

confidence: 99%

Section: In Vitro Cytotoxic Activity In Tumor Cellsmentioning

confidence: 99%

New thiazacridine agents: Synthesis, physical and chemical characterization, and in vitro anticancer evaluation

et al. 2016

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“…Mesoridazine is a neuroleptic drug used in the treatment of schizophrenia, while raloxifene is used for the treatment of osteoporosis in post-menopausal-women. 5,6 Paroxetine is an antidepressant that contains an unprotected piperidine. 7…”

Section: Introductionmentioning

confidence: 99%

Hydrogenation of functionalised pyridines with a rhodium oxide catalyst under mild conditions

Williams,

Qi,

Cox

et al. 2024

Org. Biomol. Chem.

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“…Among them, N -based heterocycles are especially important since many of the biologically active compounds such as alkaloids, glycosides, and hormones as well as some of the clinically used drugs carry N -containing heterocycles in their chemical structures. 1,2 As one of the N -based heterocycles, the piperidine ring system has been shown to possess various pharmacological effects such as antibacterial, antifungal, 3−5 anti-HIV, 6 antileishmanial, 7 anticancer, 8,9 renin inhibitory, 10 diuretic, and natriuretic 11 effects. Another N -containing heterocyclic structure, benzimidazole, is also known to have the ability to interact with biomolecules of living systems.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and antinociceptive activities of some novel benzimidazole-piperidine derivatives

Özkay¹,

Can²,

Turan³

et al. 2017

Turk J Chem

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In this study, a series of benzimidazole-piperidine derivatives were synthesized with the objective of developing potent antinociceptive agents. Some 2-(4-substituted-phenyl)-1-[2-(piperidin-1-yl)ethyl]-1 H -benzimidazole derivatives were obtained by microwave-supported reaction of an appropriate 2-(4-substituted-phenyl)-1 H -benzimidazole with 2-(piperidine-1-yl)ethyl chloride. The chemical structures of the compounds were elucidated by FT-IR, 1 H NMR, 13 C NMR, and HRMS spectral data. Antinociceptive activity was assessed by conducting hot-plate, paw-pressure, and formalin tests. Morphine (5 mg/kg, i.p) was used as a reference drug. Among the tested compounds 2a-2d and 2f -2h (10 mg/kg) increased the maximum possible effect (MPE)% values calculated for the hot-plate and paw-pressure tests and decreased the paw licking time of rats in the early phase of the formalin test, indicating centrally mediated antinociceptive activities of these derivatives. In the late-phase 2g and 2h were the only compounds reducing the paw licking duration. These data show additional peripherally mediated antinociceptive activities for these two derivatives. Falling latencies of animals in the rotarod test did not change upon the administration of test compounds; thus, the observed antinociceptive effects were specific. Predictions obtained by theoretical calculations of ADME (absorption, distribution, metabolism, excretion) properties supported the antinociceptive potential of the tested benzimidazole-piperidine derivatives.

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Synthesis, Spectral Analysis, In Vitro Microbiological Evaluation, and Molecular Docking Studies of Some Novel 1-(1-Aryl-1H-tetrazol-5-yl)-2-(piperidin-1-yl)ethanone Derivatives

Cited by 10 publications

References 17 publications

New thiazacridine agents: Synthesis, physical and chemical characterization, and in vitro anticancer evaluation

New thiazacridine agents: Synthesis, physical and chemical characterization, and in vitro anticancer evaluation

Hydrogenation of functionalised pyridines with a rhodium oxide catalyst under mild conditions

Synthesis and antinociceptive activities of some novel benzimidazole-piperidine derivatives

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